CpxRhIII/chiral carboxylic acidcatalyzed asymmetric C−H alkylation of diarylmethanamines with a diazomalonate, followed by cyclization and decarboxylation to afford 1,4‐dihydroisoquinolin‐3(2H)‐one. Secondary alkylamines as well as nonprotected primary alkylamines underwent the transformation with high enantioselectivities (up to 98.5:1.5 e.r.) by using a newly developed chiral carboxylic acid as the sole source
报告的是非手性Cp x Rh III /手性羧酸与重氮丙二酸酯催化的二芳基甲胺的不对称CH烷基化反应,然后环化和脱羧得到1,4-二氢异喹啉-3(2H)-一。通过使用新开发的手性羧酸作为唯一的手性来源,通过一致的金属化-去质子化机理实现对映选择性CH裂解,仲烷基胺和未保护的伯烷基胺都经历了高对映选择性(高达98.5:1.5 er)的转化。
SUBSTITUTED PYRIMIDINES
申请人:MERCK SHARP & DOHME CORP.
公开号:US20140235583A1
公开(公告)日:2014-08-21
The present invention relates to substituted pyrimidines useful as HIF prolyl hydroxylase inhibitors to treat anemia and like conditions.
本发明涉及取代嘧啶,用作HIF脯氨酸羟化酶抑制剂以治疗贫血和类似疾病。
PYRROLOPYRIDINE DERIVATIVE AND USE THEREOF
申请人:Takeda Pharmaceutical Company Limited
公开号:EP1535922A1
公开(公告)日:2005-06-01
A novel pyrrolopyridine derivative which is a compound represented by the formula
wherein Ring A represents an optionally substituted pyridine ring; X represents an electron-attracting group; Y represents an optionally substituted divalent C1-6 chain hydrocarbon group; R1 represents an optionally substituted hydrocarbon group; and R2 and R3 each independently represents hydrogen, an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group, or R2 and R3 may form an optionally substituted ring in cooperation with the adjacent nitrogen atom, or a salt of the compound. The pyrrolopyridine derivative has vanilloid receptor agonist activity and is useful as medicines such as a preventive/therapeutic agent and analgesic for overactive bladder.
Mapping the Active Site in a Chemzyme: Diversity in the <i>N</i>-Substituent in the Catalytic Asymmetric Aziridination of Imines
作者:Yu Zhang、Zhenjie Lu、Aman Desai、William D. Wulff
DOI:10.1021/ol802431v
日期:2008.12.4
The active site of the aziridination catalyst derived from either the VANOL or VAPOL ligand and B(OPh)(3) is larger than expected and can accommodate not only significant substitution on the diarylmethyl unit of the imine but also that alkyl (but not perfluorylalkyl) substituents on the aryl groups lead to enhanced rates and enantioselection. The screen of diarylmethyl N-substituents on the imine revealed that the 3,5-di-tert-butyldianisylmethyl group (BUDAM) gave exceptionally high asymmetric inductions for imines of aryl aldehydes.