盐酸枢复宁置于无水氯化钙,盐酸,氟化钾,无水体系中,用 乙醇 作为反应溶剂,化学反应 42.0H,以to Give 3.7 G Of Ondansetron Form B,Hcl,Kf =0.4%的收率获得产物昂丹司琼 参考文献:Novel Crystal And Solvate Forms Of Ondansetron Hydrochloride And Processes For Their Preparation 标题:Novel Crystal And Solvate Forms Of Ondansetron Hydrochloride And Processes For Their Preparation 摘要:本发明提供了新型的奥曲肽盐酸盐结晶多态形式和溶剂化物.同时还提供了制备和相互转化多态形式的过程.此外,还提供了使用新型多态形式和水合物的制药组合物和治疗方法.
专利号:US-12383499-B2 优先权日:2018-01-01 标题:Scale up synthesis of silicasome nanocarriers 发明人:NEL ANDRE E; MENG HUAN; LIU XIANGSHENG 权利人:UNIV CALIFORNIA 摘要:In order to facilitate the approval and commercialization of silicasome drug delivery systems (e.g. irinotecan silicasomes) it is necessary to scale up synthesis of the drug-loaded silicasomes. In this regard, it was discovered that the synthesis protocols used for laboratory synthesis of drug-loaded silicasomes (e.g., 500 mg/batch) do not scale to large scale silicasome production, because the resulting products were too heterogeneous for use as pharmaceuticals. Accordingly, new methods are provided herein that effectively afford the large-scale production of mesoporous silica nanoparticles (MSNPs) and lipid bilayer coated MSNPs (silicasomes).
专利号:US-8889897-B2 优先权日:2011-12-23 标 题:Electrocarboxylation synthesis for obtaining intermediates useful for the synthesis of SPAN derivatives 发明人:OSSO J ORIOL; VEGA LOURDES F; GALLARDO ILLUMINADO; GUIRADO GONZALO; GOMEZ ANA BELEN; RECHE FRANCISCA IRENE 权利人:AIR PROD & CHEM 摘要:The present invention relates to a process for obtaining a compound of formula (1), (2) or (3) by means of a electrocarboxylation with CO 2 . The present invention also relates to the new intermediates (1) and (2). The present invention further relates to the use of intermediates (1) and (2) as starting materials for the synthesis of SPAN derivatives.
专利号:US-8026375-B2 优先权日:2007-04-13 标题:Transition metal catalyzed synthesis of N-aminoindoles 发明人:HALLAND NIS; NAZARE MARC; LINDENSCHMIDT ANDREAS; RKYEK OMAR; URMANN MATTHIAS; ALONSO JORGE 权利人:SANOFI AVENTIS 摘要:The present invention relates to a process for the regioselective synthesis of compounds of the formula I, n nwherein R0; R1; R2; R3; R4; R5; R6; A1; A2; A3; A4, Q, T and J have the meanings indicated in the claims. The present invention provides a direct transition metal catalyzed process to a wide variety of multifunctional N-aminoindole or N-amino-azaindoles of the formula I from 2-halo-phenylacetylenes or (2-sulfonato)phenyl-acetylenes and N,N-disubstituted hydrazines, useful for the production of pharmaceuticals, diagnostic agents, liquid crystals, polymers, herbicides, fungicidals, nematicidals, parasiticides, insecticides, acaricides and arthropodicides.
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:US-2025206736-A1 优先权日:2019-11-14 标题 :Synthesis of kras g12c inhibitor compound 发明人:CORBETT MICHAEL THOMAS; CAILLE SEBASTIEN 权利人:AMGEN INC 摘要:The present disclosure relates to an improved, efficient, scalable process to prepare intermediate compounds, such as 2-isopropyl-4-methylpyridin-3-amine, useful for the synthesis of compounds, such as Compound 9, for the treatment of KRAS G12C mutated cancers.
专利号:US-9518034-B2 优先权日:2013-10-14 标题 :Synthesis of chiral enaminones, their derivatives, and bioactivity studies thereof 发明人:STOLTZ BRIAN M; DOUGHERTY DENNIS A; DUQUETTE DOUGLAS; DUFFY NOAH 权利人:CALIFORNIA INST OF TECHN 摘要:This invention provides enantioenriched heterocyclic enaminone compounds with quaternary stereogenic centers and novel methods of preparing the compounds. Methods include the method for the preparation of a compound of formula (I): n ncomprising treating a compound of formula (II):n n nwith a transition metal catalyst under alkylation conditions.
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合成参考文献
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