专利号:US-7230119-B2 优先权日:2004-08-25 标 题 :Process for the preparation of substituted pyrrolidine derivatives and intermediates 发明人:CHAND POORAN; EL-KATTAN YAHYA; KOTIAN PRAVIN L 权利人:BIOCRYST PHARM INC 摘要:Two syntheses are provided; one for the preparation of (3R,4R)-4-(hydroxymethyl)pyrrolidin-3-ol, and other for the preparation of (3S,4R)-4-(hydroxymethyl)pyrrolidin-3-ol. (3R,4R)-4-(hydroxymethyl)pyrrolidin-3-ol is prepared using the achiral ylide prepared from benzylamine instead of phenethylamine (Scheme 3) which provides a crystalline intermediate. The synthesis of (3S,4R)-4-(hydroxymethyl)pyrrolidin-3-ol is achieved from (S)-diethylmalate as described in Scheme 4. A process for preparing camphor sultam is also provided.
专利号:WO-2005033076-A1 优先权日:2003-10-03 标题 :Method for preparing 3-hydroxy-4-hydroxymethyl-pyrrolidine compounds 发明人:TYLER PETER CHARLES; CLINCH KEITH 权利人:IND RES LTD; TYLER PETER CHARLES; CLINCH KEITH 摘要:This invention relates to a method of preparing (3R,4R)-3-hydroxy-4-hydroxymethylpyrrolidine, a key intermediate compound for the synthesis of certain inhibitor compounds, including the step of enzyme catalysed enantioselective esterification of an hydroxy group of an hydroxypyrrolidine. The invention further relates to a method for preparing (3S,4S)-3-hydroxy-4-hydroxymethylpyrrolidine, which is the enantiomer of (3R,4R)-3-hydroxy-4-hydroxymethylpyrrolidine.
专利号:CN-109053526-A 优先权日:2018-08-13 标 题 :A chemical synthesis method of (3R,4S)-4-methylpyrrolidin-3-ylcarbamate tert-butyl hydrochloride
专利号:CN-108912032-A 优先权日:2018-08-13 标题:A chemical synthesis method of (3S, 4R)-4-methylpyrrolidin-3-ylaminomethanol tert-butyl ester hydrochloride
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