CAS: 54965-24-1; Tamoxifen Citrate

上下游产品

tamoxifen citric acid 1-(4-(2-(dimethylamino)ethoxy)phenyl)-1,2-diphenylbutan-1-ol

2-苯基丁酰苯置于盐酸,Magnesium体系中,用 四氢呋喃,水,丙酮 作为反应溶剂,化学反应 13.0H,反应生成 枸橼酸他莫昔芬
参考文献:枸橼酸他莫昔芬的工业化制备工艺
标题:枸橼酸他莫昔芬的工业化制备工艺
摘要:本发明涉及药物合成技术领域,具体涉及一种枸橼酸他莫昔芬的工业化制备工艺.所述制备工艺包括以下步骤:(1)醚化:以对溴苯酚和二甲氨基氯乙烷盐酸盐为原料,以甲苯作为反应溶剂,在氢氧化钠作用下进行醚化反应,得到醚化物;(2)格氏反应:以四氢呋喃作为反应溶剂,先将醚化物和引发剂反应得到格氏试剂,再与α‑乙基去氧苯偶姻进行格式反应,得到格氏物;(3)脱水,碱化:先将格氏物与盐酸进行脱水反应,再与氢氧化钠溶液进行碱化反应,得到他莫昔芬游离碱;(4)成盐反应:以他莫昔芬游离碱和枸橼酸为原料,以丙酮作为反应溶剂,进行成盐反应,得到枸橼酸他莫昔芬.本发明的工艺条件易于控制,产品纯度达到99.5%,产品总收率高,生产成本低.

专利信息

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-2013281742-A1
优先权日:2011-01-03
标题:Method and synthesis of initiators for telechelic polyisobutylenes
发明人：KENNEDY JOSEPH P; ERDODI GABOR
权利人:KENNEDY JOSEPH P; ERDODI GABOR; UNIV AKRON
摘要:A new methodology for the synthesis of a novel difunctional- and a known trifunctional initiator, i.e., 1,3-di(2-methoxy-2-propyl)-5-isopropyl benzene and 1,3,5-tri(2-methoxy-2-propyl)benzene, respectively, for the preparation of di- and tri-telechelic polyisobutylenes. The synthesis proceeds in three steps: 1) catalytic peroxidation of 1,3,5-triisopropylbenzene, 2) reduction of the peroxides to the corresponding alcohols, and 3) methylation of the alcohols. By controlling the conversion of the key peroxidation step the relative ratio of di- and tri-functional intermediates can be controlled. By the use of the 1,3-di(2-methoxy-2-propyl)-5-isopropyl-benzene, well-defined di-methoxy telechelic polyisobutylenes can be synthesized. Although the overall combined yield of the two initiators was only 14-20%, because of the low cost of the starting material, reagents used, and simple manipulations these compounds represent the most cost effective initiators to-date for the preparation of telechelic polyisobutylenes.

专利号:US-7893283-B2
优先权日:2004-06-04
标题:Semi-synthesis of taxane intermediates and their conversion to paclitaxel and docetaxel
发明人：NAIDU RAGINA
权利人: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 intermediates.

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.