43107-11-5Relevant articles and documents
Synthesis method of amlodipine besylate degradant impurities
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Paragraph 0032; 0033, (2018/03/01)
The invention provides a preparation method of amlodipine besylate degradant impurities. The method comprises the following steps: a) preparation of a compound 1: generating corresponding imine, namely, the compound 1 by using an acetylacetic ester compou
Optimization of activity, selectivity, and liability profiles in 5-oxopyrrolopyridine DPP4 inhibitors leading to clinical candidate (Sa)-2-(3-(aminomethyl)-4-(2,4-dichlorophenyl)-2-methyl-5-oxo-5H-pyrrolo[3,4-b] pyridin-6(7H)-yl)-N, N-dimethylacetamide (BMS-767778)
Devasthale, Pratik,Wang, Ying,Wang, Wei,Fevig, John,Feng, Jianxin,Wang, Aiying,Harrity, Tom,Egan, Don,Morgan, Nathan,Cap, Michael,Fura, Aberra,Klei, Herbert E.,Kish, Kevin,Weigelt, Carolyn,Sun, Lucy,Levesque, Paul,Moulin, Frederic,Li, Yi-Xin,Zahler, Robert,Kirby, Mark S.,Hamann, Lawrence G.
, p. 7343 - 7357 (2013/10/21)
Optimization of a 5-oxopyrrolopyridine series based upon structure-activity relationships (SARs) developed from our previous efforts on a number of related bicyclic series yielded compound 2s (BMS-767778) with an overall activity, selectivity, efficacy, PK, and developability profile suitable for progression into the clinic. SAR in the series and characterization of 2s are described.
Direct β-acyloxylation of enamines via PhIO-mediated intermolecular oxidative C-O bond formation and its application to the synthesis of oxazoles
Liu, Xin,Cheng, Ran,Zhao, Feifei,Zhang-Negrerie, Daisy,Du, Yunfei,Zhao, Kang
supporting information, p. 5480 - 5483 (2013/01/15)
A direct β-acyloxylation of enamine compounds has been achieved by using iodosobenzene (PhIO) as an oxidant to realize the intermolecular oxidative C(sp2)-O bond formation between enamines and various carboxylic acids, including N-protected amino acids. The transformation tolerates a wide range of functional groups and furnishes a variety of β-acyloxy enamines that can be conveniently converted to oxazole compounds via cyclodehydration.