Uniconazole-P的合成

Synthesis of Uniconazole P

对氯苯甲醛与α－三唑基频哪酮在ＫＦ／Ａｌ２Ｏ３／ＰＥＧ４０００存在下经Ｋｎｏｅｖｅｎａｇｅｌ反应得８５％烯基三唑酮（Ⅱ）（Ｅ／Ｚ＝０．６５），Ⅱ经光异构化得９２％Ｅ－Ⅱ（Ｅ／Ｚ≥９９／１）；Ｅ－Ⅱ在手性相转移催化剂的存在下进行选择性不对称还原得９２％Ｕｎｉｃｏｎａｚｏｌｅ－Ｐ（Ⅰ），ｅｅ＝３０％，Ｅ／Ｚ≥９９／１．Ⅰ是高效的植物生长延缓剂．

Chlorophenyl acetaldelyde reacting with α triazolylpinacolone in the presence of KF/Al 2O 3/PEG4000 will produce 85% vinyltriazolyl ketone(Ⅱ) with E/Z =0 65; Ⅱ is then isomerized by light to a yield of 92% E Ⅱ with E/Z ≥99/1. It is then reduced in the presence of certain charge transfer catalyst V by KBH 4 to 92% Uniconazole P with ee of 30%.