Category: 187035-79-6

Zheng, Yajun et al. published their research in Journal of Medicinal Chemistry in 2016 | CAS: 187035-79-6

Ethyl 2-chloro-4-(trifluoromethyl)pyrimidine-5-carboxylate (cas: 187035-79-6) belongs to pyrimidine derivatives. Heterocyclic compounds bearing the pyrimidine core are of tremendous interest as they constitute an important class of natural and synthetic compounds exhibiting diverse useful biological activities that hold attractive potential for clinical translation as therapeutic agents in alleviation of a myriad of diseases. For example, the neurotoxin tetrodotoxin is a pyrimidine derivative. It is found in a number of species including the Japanese puffer fish, the blue-ringed octopus, and the orange-bellied newt. Tetrodotoxin prevents the transmission of nerve signals and can result in paralysis and death.Name: Ethyl 2-chloro-4-(trifluoromethyl)pyrimidine-5-carboxylate

Discovery of a Novel, Orally Efficacious Liver X Receptor (LXR) β Agonist was written by Zheng, Yajun;Zhuang, Linghang;Fan, Kristi Yi;Tice, Colin M.;Zhao, Wei;Dong, Chengguo;Lotesta, Stephen D.;Leftheris, Katerina;Lindblom, Peter R.;Liu, Zhijie;Shimada, Jun;Noto, Paul B.;Meng, Shi;Hardy, Andrew;Howard, Lamont;Krosky, Paula;Guo, Joan;Lipinski, Kerri;Kandpal, Geeta;Bukhtiyarov, Yuri;Zhao, Yi;Lala, Deepak;Van Orden, Rebecca;Zhou, Jing;Chen, Guozhou;Wu, Zhongren;McKeever, Brian M.;McGeehan, Gerard M.;Gregg, Richard E.;Claremon, David A.;Singh, Suresh B.. And the article was included in Journal of Medicinal Chemistry in 2016.Name: Ethyl 2-chloro-4-(trifluoromethyl)pyrimidine-5-carboxylate This article mentions the following:

This article describes the application of Contour to the design and discovery of a novel, potent, orally efficacious liver X receptor β (LXRβ) agonist ((R)-(2-(4-(4-(hydroxymethyl)-3-(methylsulfonyl)phenyl)-2-isopropylpiperazin-1-yl)-4-(trifluoromethyl)pyrimidin-5-yl)methanol (17)). Contour technol. is a structure-based drug design platform that generates mols. using a context perceptive growth algorithm guided by a contact sensitive scoring function. The growth engine uses binding site perception and programmable growth capability to create drug-like mols. by assembling fragments that naturally complement hydrophilic and hydrophobic features of the protein binding site. Starting with a crystal structure of LXRβ and a docked 2-(methylsulfonyl)benzyl alc. fragment, Contour was used to design agonists containing a piperazine core. Compound (17) binds to LXRβ with high affinity and to LXRα to a lesser extent, and induces the expression of LXR target genes in vitro and in vivo. This mol. served as a starting point for further optimization and generation of a candidate which is currently in human clin. trials for treating atopic dermatitis. In the experiment, the researchers used many compounds, for example, Ethyl 2-chloro-4-(trifluoromethyl)pyrimidine-5-carboxylate (cas: 187035-79-6Name: Ethyl 2-chloro-4-(trifluoromethyl)pyrimidine-5-carboxylate).

Ethyl 2-chloro-4-(trifluoromethyl)pyrimidine-5-carboxylate (cas: 187035-79-6) belongs to pyrimidine derivatives. Heterocyclic compounds bearing the pyrimidine core are of tremendous interest as they constitute an important class of natural and synthetic compounds exhibiting diverse useful biological activities that hold attractive potential for clinical translation as therapeutic agents in alleviation of a myriad of diseases. For example, the neurotoxin tetrodotoxin is a pyrimidine derivative. It is found in a number of species including the Japanese puffer fish, the blue-ringed octopus, and the orange-bellied newt. Tetrodotoxin prevents the transmission of nerve signals and can result in paralysis and death.Name: Ethyl 2-chloro-4-(trifluoromethyl)pyrimidine-5-carboxylate

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Yang, Yang et al. published their research in Organic Letters in 2014 | CAS: 187035-79-6

Ethyl 2-chloro-4-(trifluoromethyl)pyrimidine-5-carboxylate (cas: 187035-79-6) belongs to pyrimidine derivatives. The pyrimidine nitrogenous bases are derived from the organic compound pyrimidine through the addition of various functional groups. For example, the neurotoxin tetrodotoxin is a pyrimidine derivative. It is found in a number of species including the Japanese puffer fish, the blue-ringed octopus, and the orange-bellied newt. Tetrodotoxin prevents the transmission of nerve signals and can result in paralysis and death.HPLC of Formula: 187035-79-6

Highly Selective Palladium-Catalyzed Cross-Coupling of Secondary Alkylzinc Reagents with Heteroaryl Halides was written by Yang, Yang;Niedermann, Katrin;Han, Chong;Buchwald, Stephen L.. And the article was included in Organic Letters in 2014.HPLC of Formula: 187035-79-6 This article mentions the following:

The highly selective palladium-catalyzed Negishi coupling of secondary alkylzinc reagents with heteroaryl halides is described [e.g., using a palladacycle precatalyst ligated by CPhos, 3-chlorobenzisothiazole was coupled with i-PrZnBr.LiCl to afford 3-isopropylbenzisothiazole in 78% yield (normal:rearranged ratio = 98:2)]. The development of a series of biarylphosphine ligands has led to the identification of an improved catalyst for the coupling of electron-deficient heterocyclic substrates. Preparation and characterization of oxidative addition complex (L)(Ar)PdBr provided insight into the unique reactivity of catalysts based on CPhos-type ligands in facilitating challenging reductive elimination processes. In the experiment, the researchers used many compounds, for example, Ethyl 2-chloro-4-(trifluoromethyl)pyrimidine-5-carboxylate (cas: 187035-79-6HPLC of Formula: 187035-79-6).

Ethyl 2-chloro-4-(trifluoromethyl)pyrimidine-5-carboxylate (cas: 187035-79-6) belongs to pyrimidine derivatives. The pyrimidine nitrogenous bases are derived from the organic compound pyrimidine through the addition of various functional groups. For example, the neurotoxin tetrodotoxin is a pyrimidine derivative. It is found in a number of species including the Japanese puffer fish, the blue-ringed octopus, and the orange-bellied newt. Tetrodotoxin prevents the transmission of nerve signals and can result in paralysis and death.HPLC of Formula: 187035-79-6

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Zheng, Yajun et al. published their research in Journal of Medicinal Chemistry in 2016 | CAS: 187035-79-6

Ethyl 2-chloro-4-(trifluoromethyl)pyrimidine-5-carboxylate (cas: 187035-79-6) belongs to pyrimidine derivatives. Heterocyclic compounds bearing the pyrimidine core are of tremendous interest as they constitute an important class of natural and synthetic compounds exhibiting diverse useful biological activities that hold attractive potential for clinical translation as therapeutic agents in alleviation of a myriad of diseases. For example, the neurotoxin tetrodotoxin is a pyrimidine derivative. It is found in a number of species including the Japanese puffer fish, the blue-ringed octopus, and the orange-bellied newt. Tetrodotoxin prevents the transmission of nerve signals and can result in paralysis and death.Name: Ethyl 2-chloro-4-(trifluoromethyl)pyrimidine-5-carboxylate

Discovery of a Novel, Orally Efficacious Liver X Receptor (LXR) β Agonist was written by Zheng, Yajun;Zhuang, Linghang;Fan, Kristi Yi;Tice, Colin M.;Zhao, Wei;Dong, Chengguo;Lotesta, Stephen D.;Leftheris, Katerina;Lindblom, Peter R.;Liu, Zhijie;Shimada, Jun;Noto, Paul B.;Meng, Shi;Hardy, Andrew;Howard, Lamont;Krosky, Paula;Guo, Joan;Lipinski, Kerri;Kandpal, Geeta;Bukhtiyarov, Yuri;Zhao, Yi;Lala, Deepak;Van Orden, Rebecca;Zhou, Jing;Chen, Guozhou;Wu, Zhongren;McKeever, Brian M.;McGeehan, Gerard M.;Gregg, Richard E.;Claremon, David A.;Singh, Suresh B.. And the article was included in Journal of Medicinal Chemistry in 2016.Name: Ethyl 2-chloro-4-(trifluoromethyl)pyrimidine-5-carboxylate This article mentions the following:

This article describes the application of Contour to the design and discovery of a novel, potent, orally efficacious liver X receptor β (LXRβ) agonist ((R)-(2-(4-(4-(hydroxymethyl)-3-(methylsulfonyl)phenyl)-2-isopropylpiperazin-1-yl)-4-(trifluoromethyl)pyrimidin-5-yl)methanol (17)). Contour technol. is a structure-based drug design platform that generates mols. using a context perceptive growth algorithm guided by a contact sensitive scoring function. The growth engine uses binding site perception and programmable growth capability to create drug-like mols. by assembling fragments that naturally complement hydrophilic and hydrophobic features of the protein binding site. Starting with a crystal structure of LXRβ and a docked 2-(methylsulfonyl)benzyl alc. fragment, Contour was used to design agonists containing a piperazine core. Compound (17) binds to LXRβ with high affinity and to LXRα to a lesser extent, and induces the expression of LXR target genes in vitro and in vivo. This mol. served as a starting point for further optimization and generation of a candidate which is currently in human clin. trials for treating atopic dermatitis. In the experiment, the researchers used many compounds, for example, Ethyl 2-chloro-4-(trifluoromethyl)pyrimidine-5-carboxylate (cas: 187035-79-6Name: Ethyl 2-chloro-4-(trifluoromethyl)pyrimidine-5-carboxylate).

Ethyl 2-chloro-4-(trifluoromethyl)pyrimidine-5-carboxylate (cas: 187035-79-6) belongs to pyrimidine derivatives. Heterocyclic compounds bearing the pyrimidine core are of tremendous interest as they constitute an important class of natural and synthetic compounds exhibiting diverse useful biological activities that hold attractive potential for clinical translation as therapeutic agents in alleviation of a myriad of diseases. For example, the neurotoxin tetrodotoxin is a pyrimidine derivative. It is found in a number of species including the Japanese puffer fish, the blue-ringed octopus, and the orange-bellied newt. Tetrodotoxin prevents the transmission of nerve signals and can result in paralysis and death.Name: Ethyl 2-chloro-4-(trifluoromethyl)pyrimidine-5-carboxylate

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Yang, Yang et al. published their research in Organic Letters in 2014 | CAS: 187035-79-6

Ethyl 2-chloro-4-(trifluoromethyl)pyrimidine-5-carboxylate (cas: 187035-79-6) belongs to pyrimidine derivatives. The pyrimidine nitrogenous bases are derived from the organic compound pyrimidine through the addition of various functional groups. For example, the neurotoxin tetrodotoxin is a pyrimidine derivative. It is found in a number of species including the Japanese puffer fish, the blue-ringed octopus, and the orange-bellied newt. Tetrodotoxin prevents the transmission of nerve signals and can result in paralysis and death.HPLC of Formula: 187035-79-6

Highly Selective Palladium-Catalyzed Cross-Coupling of Secondary Alkylzinc Reagents with Heteroaryl Halides was written by Yang, Yang;Niedermann, Katrin;Han, Chong;Buchwald, Stephen L.. And the article was included in Organic Letters in 2014.HPLC of Formula: 187035-79-6 This article mentions the following:

The highly selective palladium-catalyzed Negishi coupling of secondary alkylzinc reagents with heteroaryl halides is described [e.g., using a palladacycle precatalyst ligated by CPhos, 3-chlorobenzisothiazole was coupled with i-PrZnBr.LiCl to afford 3-isopropylbenzisothiazole in 78% yield (normal:rearranged ratio = 98:2)]. The development of a series of biarylphosphine ligands has led to the identification of an improved catalyst for the coupling of electron-deficient heterocyclic substrates. Preparation and characterization of oxidative addition complex (L)(Ar)PdBr provided insight into the unique reactivity of catalysts based on CPhos-type ligands in facilitating challenging reductive elimination processes. In the experiment, the researchers used many compounds, for example, Ethyl 2-chloro-4-(trifluoromethyl)pyrimidine-5-carboxylate (cas: 187035-79-6HPLC of Formula: 187035-79-6).

Ethyl 2-chloro-4-(trifluoromethyl)pyrimidine-5-carboxylate (cas: 187035-79-6) belongs to pyrimidine derivatives. The pyrimidine nitrogenous bases are derived from the organic compound pyrimidine through the addition of various functional groups. For example, the neurotoxin tetrodotoxin is a pyrimidine derivative. It is found in a number of species including the Japanese puffer fish, the blue-ringed octopus, and the orange-bellied newt. Tetrodotoxin prevents the transmission of nerve signals and can result in paralysis and death.HPLC of Formula: 187035-79-6

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Share a compound : 187035-79-6

At the same time, in my other blogs, there are other synthetic methods of this type of compound,187035-79-6, Ethyl 2-chloro-4-(trifluoromethyl)pyrimidine-5-carboxylate, and friends who are interested can also refer to it.

Adding a certain compound to certain chemical reactions, such as: 187035-79-6, Ethyl 2-chloro-4-(trifluoromethyl)pyrimidine-5-carboxylate, can increase the reaction rate and produce products with better performance than those obtained under traditional synthetic methods. Here is a downstream synthesis route of the compound, Product Details of 187035-79-6, blongs to pyrimidines compound. Product Details of 187035-79-6

Example 13 (R)-(2-(8-(hydroxymethyl)-1-isopropyl-7-(methylsulfonyl)-3,4-dihydrobenzo[4,5]imidazo[1,2-a]pyrazin-2(1H)-yl)-4-(trifluoromethyl)pyrimidin-5-yl)methanol and (S)-(2-(8-(hydroxymethyl)-1-isopropyl-7-(methylsulfonyl)-3,4-dihydrobenzo[4,5]imidazo[1,2-a]pyrazin-2(1H)-yl)-4-(trifluoromethyl)pyrimidin-5-yl)methanol To a solution of (R)-methyl 1-isopropyl-7-(methylsulfonyl)-1,2,3,4-tetrahydrobenzo[4,5]imidazo[1,2-a]pyrazine-8-carboxylate (80 mg, 0.228 mmol) in iPrOH (2 mL) and DCM (1 mL) was added ethyl 2-chloro-4-(trifluoromethyl)pyrimidine-5-carboxylate (174 mg, 0.684 mmol) and DIEA (177 mg, 1.37 mmol). The mixture was stirred at 60 C. overnight. Water (5 mL) was added to the mixture and the aqueous layer was extracted with EtOAc (2*10 mL). The combined organic layers were washed with water (2*10 mL) and brine, dried over anhydrous Na2SO4, filtered and concentrated under vacuum. The residue was purified by preparative TLC to afford (R)-methyl 2-(5-(ethoxycarbonyl)-4-(trifluoromethyl)pyrimidin-2-yl)-1-isopropyl-7-(methylsulfonyl)-1,2,3,4-tetrahydrobenzo[4,5]imidazo[1,2-a]pyrazine-8-carboxylate (75 mg, 57.8% yield) as a yellow solid.

At the same time, in my other blogs, there are other synthetic methods of this type of compound,187035-79-6, Ethyl 2-chloro-4-(trifluoromethyl)pyrimidine-5-carboxylate, and friends who are interested can also refer to it.

Reference:
Patent; Vitae Pharmaceuticals, Inc.; Gregg, Richard E.; (82 pag.)US2016/113930; (2016); A1;,
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Introduction of a new synthetic route about 187035-79-6

The synthetic route of 187035-79-6 has been constantly updated, and we look forward to future research findings.

In the next few decades, the world population will flourish. As the population grows rapidly and people all over the world use more and more resources, all industries must consider their environmental impact. 187035-79-6, name is Ethyl 2-chloro-4-(trifluoromethyl)pyrimidine-5-carboxylate, the common compound, a new synthetic route is introduced below. Recommanded Product: 187035-79-6

To a solution of l-isopropyl-7-(methylsulfonyl)-l,2,3,4- tetrahydrobenzo[4,5]imidazo[l,2-a]pyrazine (5.0 mg, 0.02 mmol, prepared according to example 1) in DMSO (1 mL) was added ethyl 2-chloro-4-(trifluoromethyl)pyrimidine-5- carboxylate (8.7 mg, 0.03 mmol), DIEA (6.6 mg, 0.05 mmol) under N2. The mixture was stirred at 100 C for 2 h. The mixture was diluted with water (5 mL) and extracted with EtOAc (3 x5 mL). The combined organic layers were washed with brine (5 mL), dried over anhydrous Na2S04, filtered, concentrated and then purified by preparative TLC to afford a racemic mixture of ethyl 2-(l-isopropyl-7-(methylsulfonyl)-3,4- dihydrobenzo[4,5]imidazo[l,2-a]pyrazin-2(lH)-yl)-4-(trifluoromethyl)pyrimidine-5- carboxylate (5.6 mg, 64% yield) as a white solid. LC- m/z 512.2 [M+H]+. 1H NMR (CDC13 400MHz): delta 8.98 (s, 1H), 8.07-7.98 (m, 1H), 7.93-7.83 (m, 2H), 6.16 (d, J = 6.4 Hz, 1H), 5.53-5.41 (m, 1H), 4.43-4.32 (m, 3H), 4.28-4.16 (m, 1H), 3.92-3.79 (m, 1H), 3.09 (s, 3H), 2.61-2.46 (m, 1H), 1.40 (s, 3H), 1.38-1.32 (m, 3H), 1.08 (d, J = 6.8 Hz, 3H).

The synthetic route of 187035-79-6 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; VITAE PHARMACEUTICALS, INC.; DONG, Chengguo; FAN, Yi; LEFTHERIS, Katerina; LOTESTA, Stephen; SINGH, Suresh, B.; TICE, Colin; ZHAO, Wei; ZHENG, Yajun; ZHUANG, Linghang; WO2013/138568; (2013); A1;,
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

New downstream synthetic route of 187035-79-6

At the same time, in my other blogs, there are other synthetic methods of this type of compound,187035-79-6, Ethyl 2-chloro-4-(trifluoromethyl)pyrimidine-5-carboxylate, and friends who are interested can also refer to it.

Synthetic Route of 187035-79-6, Researchers who often do experiments know that organic synthesis is a process of preparing more complex target molecules from simple raw materials through one or more chemical reactions. Generally, it requires fewer steps,and cheap raw materials. 187035-79-6, name is Ethyl 2-chloro-4-(trifluoromethyl)pyrimidine-5-carboxylate. A new synthetic method of this compound is introduced below.

The intermediate 8-(((tert-butyldiphenylsilyl)oxy)methyl)- 1 -isopropyl-7- (methylsulfonyl)- l,2,3,4-tetrahydropyrazino[l,2-a]indole was prepared following a procedure analogous to that described in Preparation 4. The mixture of compound 8-(((tert- butyldiphenylsilyl)oxy)methyl)- l-isopropyl-7-(methylsulfonyl)-l, 2,3,4- tetrahydropyrazino[l,2-a] indole (0.19 mmol), ethyl 2-chloro-4-(trifluoromethyl)pyrimidine- 5-carboxylate (97 mg, 0.38 mmol) and DIEA (100 mu,, 0.57 mmol) in j-PrOH / CH2C12 (1 mL / 0.5 mL) was stirred at 50C for 8 h. The solvent was removed under reduced pressure and the residue was purified by column chromatography on silica gel eluting with EtOAc/hexanes (1/1) to give racemic ethyl 2-(8-(hydroxymethyl)- l-isopropyl-7-(methylsulfonyl)-3,4- dihydropyrazino[ 1 ,2-a]indol-2( lH)-yl)-4-(trifluoromethyl)pyrimidine-5-carboxylate. LC- MS m/z 563 [M+Na]+. 1H NMR (400 MHz, CD3OD): delta 9.31 (s, 1H), 8.11 (s, 1H), 7.80 (s, 1H), 6.55 (s, 1H), 6.02 – 5.92 (m, 1H), 5.23 – 5.17 (m, 1H), 5.07 (s, 2H), 4.52 – 4.47 (m, 1H), 4.34 (q, J = 7.2 Hz, 2H), 4.19 – 4.06 (m, 1H), 4.00 – 3.93 (m, 1H), 3.27 (s, 3H), 2.42 – 2.32 (m, 1H), 1.36 (t, J = 7.2 Hz, 3H), 1.18 (d, J = 6.8 Hz, 3H), 1.03 (d, J = 6.8 Hz, 3H).

At the same time, in my other blogs, there are other synthetic methods of this type of compound,187035-79-6, Ethyl 2-chloro-4-(trifluoromethyl)pyrimidine-5-carboxylate, and friends who are interested can also refer to it.

Reference:
Patent; VITAE PHARMACEUTICALS, INC.; DONG, Chengguo; FAN, Yi; LEFTHERIS, Katerina; LOTESTA, Stephen; SINGH, Suresh, B.; TICE, Colin; ZHAO, Wei; ZHENG, Yajun; ZHUANG, Linghang; WO2013/138568; (2013); A1;,
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Extended knowledge of 187035-79-6

These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route,187035-79-6, its application will become more common.

Reference of 187035-79-6, In the chemical reaction process,reaction time,type of solvent,can easily affect the result of the reaction, thereby determining the yield and properties of the reaction product.An updated downstream synthesis route of 187035-79-6 as follows.

To a solution of (R)-methyl l-isopropyl-7-(methylsulfonyl)-l,2,3,4- tetrahydrobenzo[4,5]imidazo[l,2-a]pyrazine-8-carboxylate (80 mg, 0.228 mmol) in ‘PrOH (2 mL) and DCM (1 mL) was added ethyl 2-chloro-4-(trifluoromethyl)pyrimidine-5-carboxylate (174 mg, 0.684 mmol) and DIEA (177 mg, 1.37 mmol). The mixture was stirred at 60 C overnight. Water (5 mL) was added to the mixture and the aqueous layer was extracted with EtOAc (2 X 10 mL). The combined organic layers were washed with water (2 X 10 mL) and brine, dried over anhydrous Na2S04, filtered and concentrated under vacuum. The residue was purified by preparative TLC to afford (R)-methyl 2-(5-(ethoxycarbonyl)-4- (trifluoromethyl)pyrimidin-2-yl)-l-isopropyl-7-(methylsulfonyl)- 1,2,3,4- tetrahydrobenzo[4,5]imidazo[l,2-a]pyrazine-8-carboxylate (75 mg, 57.8% yield) as a yellow solid.

These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route,187035-79-6, its application will become more common.

Reference:
Patent; VITAE PHARMACEUTICALS, INC.; GREGG, Richard, E.; (143 pag.)WO2015/195922; (2015); A1;,
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Introduction of a new synthetic route about Ethyl 2-chloro-4-(trifluoromethyl)pyrimidine-5-carboxylate

According to the analysis of related databases, 187035-79-6, the application of this compound in the production field has become more and more popular.

Application of 187035-79-6, The major producers of chemicals have been the Europe, Japan and China. Due to the growing call for a cleaner, greener environment, people will have to find innovative ways to maintain their relevance. Here is a compound 187035-79-6, name is Ethyl 2-chloro-4-(trifluoromethyl)pyrimidine-5-carboxylate. This compound has unique chemical properties. The synthetic route is as follows.

(S)-(2-(8-(hydroxymethyl)-1-isopropyl-7-(methylsulfonyl)-3,4-dihydrobenzo[4,5]imidazo[1,2-a]pyrazin-2(1H)-yl)-4-(trifluoromethyl)pyrimidin-5-yl)methanol To a solution of (R)-methyl 1-isopropyl-7-(methylsulfonyl)-1,2,3,4-tetrahydrobenzo[4,5]imidazo[1,2-a]pyrazine-8-carboxylate (80 mg, 0.228 mmol) in iPrOH (2 mL) and DCM (1 mL) was added ethyl 2-chloro-4-(trifluoromethyl)pyrimidine-5-carboxylate (174 mg, 0.684 mmol) and DIEA (177 mg, 1.37 mmol). The mixture was stirred at 60 C. overnight. Water (5 mL) was added to the mixture and the aqueous layer was extracted with EtOAc (2*10 mL). The combined organic layers were washed with water (2*10 mL) and brine, dried over anhydrous Na2SO4, filtered and concentrated under vacuum. The residue was purified by preparative TLC to afford (R)-methyl 2-(5-(ethoxycarbonyl)-4-(trifluoromethyl)pyrimidin-2-yl)-1-isopropyl-7-(methylsulfonyl)-1,2,3,4-tetrahydrobenzo[4,5]imidazo[1,2-a]pyrazine-8-carboxylate (75 mg, 57.8% yield) as a yellow solid.

According to the analysis of related databases, 187035-79-6, the application of this compound in the production field has become more and more popular.

Reference:
Patent; Vitae Pharmaceuticals, Inc.; Gregg, Richard E.; US2015/250787; (2015); A1;,
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia