专利号:US-4427587-A 优先权日:1982-11-10 标 题:Total synthesis of antitumor antibiotics BBM-2040A and BBM-2040B 发明人:KANEKO TAKUSHI; WONG HENRY S L 权利人:BRISTOL MYERS CO 摘要:A new chemical synthesis of the pyrrolobenzodiazepine antibiotics BBM-2040A and B is disclosed. The disclosed total synthesis uses readily available starting materials and provides a useful alternative to the microbiological procedure previously used to prepare these antibiotics.
专利号:US-2008125587-A1 优先权日:2006-05-25 标 题 :Synthesis of triazole compounds that modulate HSP90 activity 发明人:CHIMMANAMADA DINESH U; LEE CHI-WAN; JAMES DAVID; ZHANG SHIJIE; YING WEIWEN; CHAE JUNGHYUN; PRZEWLOKA TERESA 权利人:CHIMMANAMADA DINESH U; LEE CHI-WAN; JAMES DAVID; ZHANG SHIJIE; YING WEIWEN; CHAE JUNGHYUN; PRZEWLOKA TERESA 摘要:The present invention provides novel methods of preparing triazole compounds which inhibit the activity of Hsp90. One embodiment of the invention is directed to methods for preparing a triazole compound represented by the following Structural Formula: n n n n n n n n n n or a tautomer, a pharmaceutically acceptable salt, solvate, or clathrate, or a prodrug thereof, comprising the steps of: a) reacting an amide represented by the following Structural Formula: n n n n n n n n n n with a thionation reagent to form a thioamide; b) reacting the thioamide of step a) with hydrazine to form a hydrazonamide; c) reacting the hydrazonamide of step b) with a carbonylation or a thiocarbonylation reagent. n In one embodiment, the present invention is a method of synthesis of a compound of formula (IA) n n n n n n n n n n or a tautomer, a pharmaceutically acceptable salt, solvate, or clathrate, or a prodrug thereof, comprising reacting a compound of formula (IIA) n n n n n n n n n n with an oxidizing agent, thereby producing a compound of formula (IA). n The present invention is also directed to a method of preparing a compound or a tautomer thereof represented by the following Structural Formula: n n n n n n n n n n or a tautomer, a pharmaceutically acceptable salt, solvate, or clathrate, or a prodrug thereof. The method comprises the step of reacting a first starting compound represented by the following Structural Formula: n n n n n n n n n n in the presence of a mercuric salt, with a second starting compound represented by the following Structural Formula:
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-12391691-B2 优先权日:2018-11-16 标题:Synthesis of key intermediate of KRAS G12C inhibitor compound 发明人:PARSONS ANDREW THOMAS; COCHRAN BRIAN MCNEIL; POWAZINIK IV WILLIAM; CAPORINI MARC ANTHONY 权利人:AMGEN INC 摘要:The present invention relates to an improved, efficient, scalable process to prepare intermediate compounds, such as compound 5M, having the structure n nuseful for the synthesis of compounds that target KRAS G12C mutations, such as
专利号:WO-0132645-A1 优先权日:1999-11-04 标题:The synthesis of extended bis(ethylenedithio)tetrathiafulvalene derivatives and their dihydroxyl analogues 发明人:OZTURK TURAN; TURKSOY FIGEN; WALLIS JOHN D; UMIT TUNCA 权利人:TUBITAK MARMARA RES CT; OZTURK TURAN; TURKSOY FIGEN; WALLIS JOHN D; UMIT TUNCA 摘要:The present invention describes the synthesis of six novel derivatives of bis(ethylenedithio)tetrathiafulvalene (BEDT-TTF), utilising the recently developed reaction of 1,8-diketones with Lawesson's reagent. These new BEDT-TTF derivatives (1)-(6) have potential to delocalise the positive charges formed during change-transfer salts to the peripheral. In addition to their positive charge delocalisation feature, the compounds (1)-(3) have the potential of being introduced hydrogen bonding groups and the compound (4)-(6) already have hydrogen bonding hydroxyl groups. All the new BEDT-TTF (7) derivatives described in this invention have shown comparative CV measurements with the BEDT-TTF. Each of these bis(ethylenedithio)tetrathiafulvalene derivatives of the present invention has a unique and novel structure which can not be found in the prior art and is useful for the development of new organic charge-transfer complexes.
专利号:US-10155772-B2 优先权日:2010-07-08 标题:Process for the synthesis of substituted morphinans 发明人:DUNCAN SCOTT 权利人:ALKERMES PHARMA IRELAND LTD 摘要:The invention further relates to a process for the synthesis of 3-carboxamide substituted morphinans where a 3-cyano substituted 6-oxo substituted morphinan is reacted with a 1,3-diol.
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合成参考文献
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