专利号:US-5468876-A 优先权日:1986-05-22 标题:Intermediates for the stereoconservative synthesis of 1-substituted (S)-and (R)-2-aminomethylpyrrolidines 发明人:FEDERSEL HANS-JUEGEN; HOE THOMAS; RAEMSBY STEN I; STROEM PETER H E 权利人:ASTRA AB 摘要:Disclosed are (R)- and (S)-isomers of the compounds of the Formulas II and III with at least 95% optical purity ##STR1## wherein R 1 and R 2 are the same or different and represent a hydrogen atom, a lower alkyl, lower alkenyl or lower alkynyl group, a cycloalkyl group or a group (CH 2 ) m Ph, wherein m is 0-3 and Ph is a substituted or unsubstituted phenyl group. n These compounds are intermediates in the stereoconservative synthesis of 1-substituted (S)- and (R)-2-aminomethylpyrrolidines.
专利号:US-9365587-B2 优先权日:2008-12-11 标 题:Synthesis of carbamoylpyridone HIV integrase inhibitors and intermediates 发明人:YOSHIDA HIROSHI; TAODA YOSHIYUKI; JOHNS BRIAN ALVIN; KAWASUJI TAKASHI; NAGAMATSU DAIKI 权利人:SHIONOGI & CO; VIIV HEALTHCARE CO 摘要:The invention is a process for the preparation of a compound of the following formula (I): n nwherein R is —CHO, —CH(OH) 2 or —CH(OH)(OR 4 ); P 1 is H or a hydroxyl protecting group; P 3 is H or a carboxy protecting group; R 3 is H, halogen, hydroxy, optionally substituted lower alkyl, optionally substituted cycloalkyl, etc.; R x is H, halogen or R 2 —X—NR 1 —C(O)—; etc. as defined in the specification. The compounds are useful as intermediates in synthesizing compounds having HIV integrase inhibitory activity.
专利号:WO-2019012000-A1 优先权日:2017-07-12 标题:NEW SYNTHESIS OF INTERMEDIATES FOR THE PREPARATION OF ALPHA-TOCOPHEROL
专利号:WO-8707271-A1 优先权日:1986-05-22 标 题 :A stereoconservative synthesis of 1-substituted (s)- and (r)-2-aminomethylpyrrolidines and intermediates thereto
专利号:US-8754214-B2 优先权日:2008-12-11 标题 :Synthesis of carbamoylpyridone HIV integrase inhibitors and intermediates
专利号:FI-880265-A7 优先权日:1986-05-22 标题 :Efficient stereostructure preserving synthesis of 1-substituted (S)- and (R)-2-aminomethylpyrrolidines and their intermediates
参考文献:10.1007/bf00210782 摘要:Stewart DJ, Raaphorst GP, Yau J, Beaubien AR. Active vs. passive resistance, dose-response relationships, high dose chemotherapy, and resistance modulation: a hypothesis. Invest New Drugs. 1996;14(2):115–30. doi: 10.1007/bf00210782.