Process for the preparation of enantiomerically and diastereomerically enriched cyclobutane amines and amides

专利申请号：TW107140609

公 开 号：TW201936558(A)

发 明 人：DUMEUNIER, RAPHAEL 督门尤尼尔　瑞菲尔 督門尤尼爾　瑞菲爾 SMEJKAL, TOMAS 斯美洁卡尔　托玛斯 斯美潔卡爾　托瑪斯 MISHRA, BRIJNANDAN PREMNATH 密希拉　布南登　皮姆南史 密希拉　布南登　皮姆南史 GOPALSAMUTHIRAM, VIJAYAGOPAL RAMAN 勾保萨穆瑟曼　维嘉普尔　拉曼恩 勾保薩穆瑟曼　維嘉普爾　拉曼恩 GODINEAU, EDOUARD 格顶娜　爱度亚 格頂娜　愛度亞 O'SULLIVAN, ANTHONY CORNELIUS 欧苏利文恩　安东尼　科尼利厄斯 歐蘇利文恩　安東尼　科尼利厄斯 

申 请 日：20190916

公 开 日：20181115

专利主分类号：C07B2200/07

摘      要：The present invention relates to a process for the preparation of enantiomerically and diastereomerically enriched cyclobutane amines and amides by reacting (a) cyclopropylcarbonitrile to a cyclopropylcarbaldehyde, (b) further reacting to a cyclobutanone, or (d’) further reacting to an enamide, (c) further reacting to enantiomerically and diastereomerically enriched cyclobutane amines, or (d) further reacting to an enamide and (e) to an enantiomerically and diastereomerically enriched cyclobutylamide to obtain (f) an enantiomerically and diastereomerically enriched cyclobutane amine, and (g) further reacting to an enantiomerically and diastereomerically enriched cyclobutane amide.