Category: 85386-20-5

Moriya, Minoru et al. published their patent in 2004 |CAS: 85386-20-5

The Article related to aminoquinoline preparation mch melanin concentrating hormone receptor antagonist, antiobesity aminoquinoline preparation mch melanin concentrating hormone receptor antagonist, antidiabetic agent aminoquinoline preparation mch receptor antagonist and other aspects.Recommanded Product: 5-Phenylpyrimidine-2-carboxylic acid

On December 2, 2004, Moriya, Minoru; Suzuki, Takao; Ishihara, Akane; Iwaasa, Hisashi; Kanatani, Akio published a patent.Recommanded Product: 5-Phenylpyrimidine-2-carboxylic acid The title of the patent was Preparation of pyrimidine derivatives having 2-aminoquinoline moiety as MCH receptor antagonists. And the patent contained the following:

Title compounds I [R1, R2 = alkyl, etc.; R3, R4, R6, R7 = H, alkyl, etc.; R5 = H, alkyl; R8 = halo, etc.; n = 0-4] were prepared For example, hydrogenation of nitro compound (R)-II followed by acylation with 5-phenylpyrimidine-2-carboxylic acid afforded compound (R)-III. In MCH (melanin concentrating hormone) binding assays, the IC50 value of compound (R)-III was 4.1 nM. Compounds I are claimed useful for the treatment of obesity, diabetes, etc. The experimental process involved the reaction of 5-Phenylpyrimidine-2-carboxylic acid(cas: 85386-20-5).Recommanded Product: 5-Phenylpyrimidine-2-carboxylic acid

The Article related to aminoquinoline preparation mch melanin concentrating hormone receptor antagonist, antiobesity aminoquinoline preparation mch melanin concentrating hormone receptor antagonist, antidiabetic agent aminoquinoline preparation mch receptor antagonist and other aspects.Recommanded Product: 5-Phenylpyrimidine-2-carboxylic acid

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

A new synthetic route of 85386-20-5

The chemical industry reduces the impact on the environment during synthesis 85386-20-5, I believe this compound will play a more active role in future production and life.

Application of 85386-20-5, With the rapid development and complex challenges of chemical substances, the synthesis of new drugs is usually one of the most effective ways to increase yield.85386-20-5, name is 5-Phenylpyrimidine-2-carboxylic acid, molecular formula is C11H8N2O2, molecular weight is 200.19, as common compound, the synthetic route is as follows.

To a solution of the compound as obtained in Referential Example 3 (10.2 g) in tetrahydrofuran (150 ml), 20% palladium hydroxide-on-carbon (4.19 g) was added in nitrogen atmosphere, followed by an overnight’s stirring in hydrogen atmosphere of one atmospheric pressure. The reaction system was nitrogen-exchanged to suspend the reaction, and the reaction liquid was filtered with Celite. The filtrate was concentrated under reduced pressure. To a solution of the residue in dimethylformamide (70 ml), phenylpyrimidinecarboxylic acid (5.97 g) as obtained in Referential Example 10 and triethylamine (8.3 ml) were added at 0C, followed by further dropwise addition of a solution of 2-chloro-1,3-dimethylimidazolium chloride (6.55 g) in dimethylformamide (30 ml) and subsequent an hour’s stirring. After addition of aqueous sodium hydrogencarbonate solution to the reaction liquid and dilution with water, the formed solid was recovered by filtration. The solid was subjected to silica gel column chromatography (chloroform: methanol = 95:5) and recrystallized from ethyl acetate, to provide the title compound (7.65 g) as yellow crystals. 1H-NMR(400MHz,d6-DMSO,deltappm):1.05-1.08(6H,m), 2.05-2.25(2H,m), 2.78(3/2H,s), 2.96(3/2H,s), 2.82-3.10(1H,m), 3.35-3.55(2H,m), 3.65-3.87(2H,m), 4.78-4.89(1/2H,m), 5.13-5.25(1/2H,m), 6.88-6.93(1H,m), 7.51-7.60(4H,m), 7.90-7.92(3H,m), 8.01(1H,d,J=8.8Hz), 8.36(1H,d,J=2.4Hz), 9.34(2H,s), 10.85(1H,s). ESI-MS Found:m/z 496[M+H]+

The chemical industry reduces the impact on the environment during synthesis 85386-20-5, I believe this compound will play a more active role in future production and life.

Reference:
Patent; BANYU PHARMACEUTICAL CO., LTD.; EP1630162; (2006); A1;,
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia