On October 20, 2011, Barba, Oscar; Gattrell, William; Smyth, Donald; Swain, Simon published a patent.Recommanded Product: 596114-50-0 The title of the patent was Preparation of 3-substituted 5-(pyrrolidine-1-carbonyl)pyrrolidine and its derivatives for use in the treatment of metabolic disorders. And the patent contained the following:
The title compounds I [p, q = 1-2; Z = NC(O)OR4, NC(O)NR4R5, N-heteroaryl, etc.; Y = CH2, CF2, CHF, O, NR1, C(O) or B (wherein B = 5-membered heteroaryl containing one or more heteroatoms selected from N, O and S); when Y = CH2, CF2, CHF, O, NR1 or C(O), X = (un)branched alkylene; or when Y = O or NR1, X may also be -ACHR2- (wherein A = 5-membered heteroaryl containing one or more heteroatoms selected from N, O and S); and when Y = B, X = OCHR3; Ar = (un)substituted para-substituted 6-membered heteroaryl containing one or two N atoms; R1-R3 = H, alkyl; R4 = aryl, heteroaryl, alkyl,(un)substituted cycloalkyl; R5 = H or alkyl; V = II (T = CH2, or, when m = 1, T may also be S; when T = CH2, R6 = F or CN, and when T = S, R6 = CN; R7 = H, alkyl; m = 0-1; s = 0-2); n = 0-1] which have activity as agonists of GPR119 and are useful for the treatment of metabolic disorders including type II diabetes, were prepared For example, Pd-catalyzed coupling 2-bromo-5-{3-[1-(3-isopropyl-[1,2,4]oxadiazol-5-yl)piperidin-4-yl]propoxy}pyridine with tert-Bu (2S,4S)-4-amino-2-(pyrrolidine-1-carbonyl)pyrrolidine-1-carboxylate (preparations given) followed by Boc-deprotection afforded (2S,4S)-III. Compounds I produced a concentration-dependent increase in intracellular cAMP level and generally had an EC50 of <10 μM when tested in GPR119 cAMP assay. All exemplified compounds I showed activity in DPP-IV assay having an IC50 of <20 μM. Pharmaceutical composition comprising compound I is disclosed. The experimental process involved the reaction of 2-Chloro-5-isopropylpyrimidine(cas: 596114-50-0).Recommanded Product: 596114-50-0
The Article related to pyrrolidinecarbonylpyrrolidine preparation glucose dependent insulinotropic polypeptide receptor gpr119 agonist, metabolic disorder type ii diabetes treatment pyrrolidinecarbonylpyrrolidine preparation, antidiabetic pyrrolidinecarbonylpyrrolidine preparation gpr119 agonist dipeptidyl peptidase dppiv modulator and other aspects.Recommanded Product: 596114-50-0
Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia