3-溴-1-丙醇置于ph4Sbome体系中,用 1,2-二氯乙烷 作为反应溶剂,化学反应 24.0H,以59%的收率获得产物三甲氧基酯 参考文献:The Synthesis Of Oxiranes And Oxetanes From 1,2-Or 1,3-Halohydrins Using Organoantimony(V) Alkoxide 标题:The Synthesis Of Oxiranes And Oxetanes From 1,2-Or 1,3-Halohydrins Using Organoantimony(V) Alkoxide 摘要:四苯基锑甲氧基化合物(1)是合成氧杂环烷烃和氧杂环丙烷的有效试剂,分别来自相应的1,2-和1,3-卤醇.由于反应条件为中性,含有酯基的氧杂环烷烃未经历溶解,得以完整获得.此外,在温和的条件下(60-80oc),氧杂环丙烷的制备虽然通常不容易,但也能得到非常好的产率. DOI:10.1055/s-1990-26800
专利号:US-12421534-B2 优先权日:2021-11-10 标 题 :Engineered enzymes and method for the synthesis of diverse tyrosine analogs 发明人:ALMHJELL PATRICK J; ARNOLD FRANCES H 权利人:CALIFORNIA INST OF TECHN 摘要:Provided herein is an engineered tryptophan synthase β-subunit (TrpB) that catalyzes the synthesis of tyrosine, tyrosine analogs, or salts thereof. Also provided herein are methods for preparing tyrosine, tyrosine analogs, or a salt thereof using the engineered TrpB described herein.
专利号:US-8293930-B1 优先权日:2004-06-25 标题 :One pot synthesis of taxane derivatives and their conversion to paclitaxel and docetaxel 发明人:NAIDU RAGINA 权利人:NAIDU RAGINA; CHATHAM BIOTEC LTD 摘要:A process is provided for the semi-synthesis of taxane intermediates useful in the preparation of paclitaxel and docetaxel, in particular, the semi-synthesis of protected taxane intermediate in a one pot reaction of protecting the C-7 and C-10 positions and attaching a side chain at the C-13 position and subsequently deprotecting the group to form paclitaxel or docetaxel, and taxane intermediates.
专利号:US-2004266827-A1 优先权日:2003-06-25 标 题 :Convergent asymmetric route to produce a key intermediate towards the synthesis of a garft inhibitor 发明人:NOTZ WOLFGANG REINHARD LUDWIG; MARTINEZ CARLOS ALBERTO 权利人:AGOURON PHARMA 摘要:The invention relates to processes for the preparation of a key intermediate in the synthesis of a GARFT inhibitor of formula (Ia) containing a 4-methyl-substituted thiophene core: n n n wherein said key intermediate has the following formula (I): n n n wherein each of R 1 and R 2 are independently a moiety that together with the attached CO 2 forms a readily hydrolyzable ester group; n from a compound of the formula (VI): n n n wherein R 1 is as described above, Pg 1 is an amino protecting group, and Pg 2 is an ether protecting group; wherein said processes are as described in the specification.
专利号:US-6576777-B2 优先权日:1996-10-18 标 题:Semi-synthesis of a protected baccatin III compound 发明人:ZAMIR LOLITA; CARON GAETAN 权利人:INST NAT RECH SCIENT 摘要:The present invention relates to a semi-synthetic process to convert a naturally occurring taxane into a suitable starting material for the synthesis of paclitaxel and related compounds. Specifically, the present invention relates to a process for the conversion of 9-dihydro-13-acetylbaccatin III into a 7-protected baccatin III which can then be used as starting material for the synthesis of taxane derivatives such as paclitaxel, docetaxel, cephalomannine and other taxanes structurally related to baccatin III. The method as described uses a preparative scale technique which is amenable to commercial scale-up.
专利号:WO-2008032104-A1 优先权日:2006-09-15 标题:One pot synthesis of taxane derivatives and their conversion to paclitaxel and docetaxel 发明人:WALKER ROSS THOMSON; NAIDU RAGINA 权利人:CHATHAM BIOTEC LTD; WALKER ROSS THOMSON; NAIDU RAGINA 摘要:A process is provided for the semi-synthesis of taxane intermediates useful in the preparation of paclitaxel and docetaxel, in particular, the semi-synthesis of protected taxane intermediate in a one pot reaction, of protecting the C-10 and attaching a side chain at C-13 position and subsequently deprotecting the group to form paclitaxel or docetaxel, and intermediates used therein.
专利号:WO-0134589-A1 优先权日:1999-11-05 标 题 :Semi-synthesis of baccatin iii from 9-dihydro-13-acetylbaccatin iii 发明人:ZAMIR LOLITA 权利人:ZAMIR LOLITA 摘要:The present invention relates to a semi-synthetic process to convert a naturally occurring taxane into a suitable starting material for the synthesis of paclitaxel and related compounds. Specifically, the present invention relates to a process for the conversion of 9-dihydro-13-acetylbaccatin III into baccatin III which can then be used as starting material for the synthesis of taxane derivatives such as paclitaxel, docetaxel, cephalomannine and other taxanes structurally related to baccatin III.