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-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-2017327504-A1 优先权日:2014-10-30 标 题:Synthesis of Substituted 1H-Pyrazolo[3,4-D]Pyrimidines 发明人:ROSE CHRISTOPHER; SILBERGER HERBERT; SCHREINER ERWIN; FELZMANN WOLFGANG; MARAS NENAD 权利人:SANDOZ AG 摘要:The present invention refers to the synthesis and intermediates of substituted bicyclic compounds by using a central 1H-pyrazolo[3,4-d]pyrimidine of formula (I), which is assembled starting from 4,6-dichloropyrimidine carboxylic acid. The invention in particular refers to the synthesis of the Bruton's tyrosine kinase (Btk) inhibitor 1-((R)-3-(4-amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-en-1-one(ibrutinib) and its synthesis intermediates.
专利号:US-10730904-B2 优先权日:2012-11-14 标 题:Method for liquid-phase synthesis of nucleic acid 发明人:NONOGAWA MITSURU; NAGATA TOSHIAKI; SAITO HIDEKI; YASUMA TSUNEO 权利人:TAKEDA PHARMACEUTICALS CO 摘要:In this method, an oligonucleotide represented by formula (II) [wherein Y 1 , Q, Base, r and r′ are each as defined in claim 1 ] is prepared by using, as a synthesis unit, a novel nucleoside monomer compound represented by formula (I) [wherein X, R 1 , Y, Base, Z, Ar, R 2 , R 3 and n are each as defined in claim 1 ]. The novel nucleoside monomer compound is a nucleoside, the base moiety of which is substituted with an aromatic-hydrocarbon-ring-carbonyl or -thiocarbonyl group having at least one hydrophobic group. The method can dispense with column-chromatographic purification in every reaction, and enables base elongation not only in the 3′-direction but also in the 5′-direction, thus attaining efficient liquid-phase mass synthesis of an oligonucleotide.
专利号:US-2005192445-A1 优先权日:2004-03-01 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:PHYTOGEN LIFE SCIENCES INC 摘要:A process is provided for the semi-synthesis of taxane intermediates and aziridine analogues of cephalomannne and baccatin III intermediates, and the conversion of such intermediates and analogues to paclitaxel and docetaxel.
专利号:US-9994508-B2 优先权日:2012-12-11 标 题:Versatile and functionalised intermediates for the synthesis of vitamin D and novel vitamin D derivatives 发明人:LOPEZ PEREZ BORJA; SIGUEIRO PONTE RITA; MAESTRO SAAVEDRA MIGUEL A; MOURINO MOSQUERA ANTONIO 权利人:ENDOTHERM GMBH 摘要:Novel intermediates for the complete synthesis of vitamin D are provided that allow a great versatility of functional groups in the final vitamin derivatives. Vitamin derivatives that are epimeric in position 3 and vitamin derivatives with a wide range of functionalities in position 18, including compounds with isotopic labelling are provided.
摘要:Hardman-Baldwin, A. M.; Mattson, A. E., Science of Synthesis Knowledge Updates, (2017) 1, 217. 摘要:Hardman-Baldwin, A. M.; Mattson, A. E., Science of Synthesis Knowledge Updates, (2017) 1, 218. 摘要:Hardman-Baldwin, A. M.; Mattson, A. E., Science of Synthesis Knowledge Updates, (2017) 1, 216. 摘要:Hardman-Baldwin, A. M.; Mattson, A. E., Science of Synthesis Knowledge Updates, (2017) 1, 230. 摘要:Hardman-Baldwin, A. M.; Mattson, A. E., Science of Synthesis Knowledge Updates, (2017) 1, 223.