三氯乙酸甲酯置于copper Acetylacetonate,亚磷酸氢二甲酯体系中,用21%的收率获得二氯乙酸甲酯 参考文献:Polozov,A. M.; Mustafin,A. Kh.,Journal Of General Chemistry Of The Ussr,1992,Vol. 62,# 5.1,P. 850-852 标题:Polozov,A. M.; Mustafin,A. Kh.,Journal Of General Chemistry Of The Ussr,1992,Vol. 62,# 5.1,P. 850-852
专利号:US-6504041-B2 优先权日:1996-11-15 标题 :Synthesis of ruthenium or osmium metathesis catalysts 发明人:GRUBBS ROBERT H; BELDERRAIN TOMAS R; BROWN SETH N; WILHELM THOMAS E 权利人:CALIFORNIA INST OF TECHN 摘要:The present invention relates to the synthesis of highly active ruthenium and osmium carbene metathesis catalyst in good yield from readily available starting materials. The catalysts that may be synthesized are of the general formula n wherein: n M is ruthenium or osmium; n X and X 1 are independently any anionic ligand; n L and L 1 are any neutral electron donor ligand; and, n R and R 1 are each hydrogen or one of the following substituent groups: C 2 -C 20 alkenyl, C 2 -C 20 alkynyl, C 1 -C 20 alkyl, aryl, C 1 -C 20 carboxylate, C 1 -C 20 alkoxy, C 2 -C 20 alkenyloxy, C 2 -C 20 alkynyloxy, aryloxy, C 2 -C 20 alkoxycarbonyl, C 1 -C 20 alkylthio, C 1 -C 20 alkylsulfonyl and C 1 -C 20 alkylsulfinyl. Optionally, the substituent group may be substituted with one or more groups selected from C 1 -C 5 alkyl, halogen, C 1 -C 5 alkoxy, and aryl. When the substitute aryl group is phenyl, it may be further substituted with one or more groups selected from a halogen, a C 1 -C 5 alkyl, or a C 1 -C 5 alkoxy. Specific synthetic protocols for vinyl alkylidene catalysts wherein R is hydrogen and R 1 is —CHCR 12 R 13 and non-vinyl alkylidene catalysts are also disclosed. In addition to the ease of synthesis (typically a one-step synthesis), the reactions generally may be run at or above room temperature and the resulting products usually may be used without extensive post synthesis purification.
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:WO-2016113764-A4 优先权日:2015-01-15 标题:One step process for the synthesis of azido alcohols from alkene 发明人:SUDALAI ARUMUGAM; PRASAD PRAGATI KISHORE; REDDI RAMBABU 权利人:COUNCIL SCIENT IND RES 摘要:The present invention relates to one step room temperature process for the synthesis of azido alcohols from alkenes. More particularly, I 2 catalysed a regio and diastereo selective one step room temperature process for the synthesis of 1,2-azido alcohols from alkenes.
专利号:US-7585986-B2 优先权日:2004-02-24 标题 :Semi-synthesis of taxane intermediates and aziridine analogues 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 and aziridine analogues of cephalomannine and baccatin III intermediates, and the conversion of such intermediates and analogues to paclitaxel and docetaxel.
专利号:US-7838694-B2 优先权日:2004-04-23 标题 :Semi-synthesis and isolation of taxane intermediates from a mixture of taxanes 发明人:NAIDU RAGINA; FOO SAMUEL SIANG KIANG 权利人:CHATHAM BIOTEC LTD 摘要:A process is provided for the semi-synthesis and isolation of taxane intermediates useful in the preparation of paclitaxel and docetaxel, in particular, the semi-synthesis and isolation of 10-deacetylbaccatin III, the semi-synthesis of a mixture of 10-deacetylbaccatin III and baccatin III, and protected derivatives thereof, from a mixture of taxanes.
专利号:US-7906661-B2 优先权日:2004-06-29 标 题 :Semi-synthetic conversion of paclitaxel to docetaxel 发明人:NAIDU RAGINA; FOO SAMUEL SIANG KIANG; XUE BAOYU; FAN BO 权利人:CHATHAM BIOTEC LTD 摘要:A process is provided for the semi-synthesis of taxane derivatives useful in the preparation of docetaxel, in particular, the semi-synthesis of protected taxane derivatives in a one pot reaction of protecting the C-2′, C-7 and C-10 positions and introducing a t-Boc group at the nitrogen of the amide group at the C-3′ position in paclitaxel and subsequently conversion to docetaxel, and derivatives used therein.