Enantioselective Friedel-Crafts Alkylation of Thiophenes with Ethyl Glyoxylate: Easy Access to Chiral Secondary Alcohols
作者:Zhong Huang、Jingchang Zhang、Yuqiang Zhou、Nai-Xing Wang
DOI:10.1002/ejoc.201001455
日期:2011.2
Friedel–Craftsalkylation reactions of ethylglyoxylate with various thiophenes to give the corresponding chiralsecondaryalcohols were demonstrated. The majority of these reactions proceeded with good enantioselectivities (up to 91 %) and satisfactory isolated yields. Notably, we found that 2-substituted thiophenes underwent the reaction more smoothly than unsubstituted and 3-substituted thiophenes
PROCESS FOR PREPARATION OF CLOPIDOGREL BISULPHATE FORM-1
申请人:ALLA Venkat Reddy
公开号:US20070191609A1
公开(公告)日:2007-08-16
Disclosed herein is a cost effective and industrially feasible process for the preparation of (+) Clopidogrel bisulphate. The present invention further discloses a novel method of precipitation of (+) Clopidogrel bisulphate Form I directly from solvent mix of methanol and acetone in presence of sulfuric acid at a temperature of 25-40° C.
[EN] PROCESS FOR PREPARATION OF CLOPIDOGREL BISULFATE FORM 1<br/>[FR] PROCÉDÉ DE SYNTHÈSE DE LA FORME 1 DU CLOPIDOGREL BISULFATE
申请人:LEE PHARMA LTD
公开号:WO2007094006A1
公开(公告)日:2007-08-23
[EN] Disclosed herein is cost effective and industrially feasible process for the preparation of (+) Clopidogrel bisulfate. The present invention further discloses a novel method of precipitation of (+) Clopidogrel bisulfate Form I directly from solvent mix of methanol and acetone in presence of sulfuric acid at a temperature of 25-40° C [FR] La présente invention a pour objet un procédé rentable et transposable à l'échelle industrielle de synthèse du (+)-Clopidogrel bisulfate. La présente invention concerne en outre une nouvelle méthode de précipitation de la Forme I du (+)-Clopidogrel bisulfate directement à partir du mélange de solvants méthanol/acétone en présence d'acide sulfurique à une température comprise entre 25 et 40 °C.
The study of Friedel–Crafts alkylation reaction of thiophenes with glyoxylate imine catalyzed by Fe(III): an easy access to α-aminoesters
作者:Zhong Huang、Jingchang Zhang、Nai-Xing Wang
DOI:10.1016/j.tet.2011.01.039
日期:2011.3
A Friedel–Craftsalkylation reaction of thiophenes with glyoxylate imine was developed to give α-aminoesters. In the presence of FeCl3·6H2O as the catalyst, various α-aminoesters were prepared with moderate to high yields (up to 95%) except for some special substrates.