专利号:US-7288661-B2 优先权日:2003-12-10 标 题 :Process for the synthesis of (2S,3aS,7aS)-1-[(S)-alanyl]-octahydro-1H-indole-2-carboxylic acid compounds and application in the synthesis of perindopril 发明人:DUBUFFET THIERRY; LECOUVE JEAN-PIERRE 权利人:SERVIER LAB 摘要:Process for the synthesis of compounds of formula (I): n nwherein R represents a hydrogen atom or a protecting group for the amino function.n n Application in the synthesis of perindopril and pharmaceutically acceptable salts thereof.
专利号:US-7173021-B2 优先权日:2004-09-02 标题:Synthesis of temozolomide esters as potent anticancer pro-drugs for topical and transdermal applications in treatments of cancers 发明人:WANG YONGFENG; CONWAY BARBARA R; SUPPASANSATORN PANASSAYA 权利人:TIANJIN NORTH PHARM SCI TECH C 摘要:This invention relates to the use of temozolomide esters (4-dihydro-3-methyl-4-oxoimidazo[5,1-d]-1,2,3,5-tetrazine-8-carboxylate esters) Formula 1 as potent anticancer pro-drugs for treatment of cancers by topical and transdermal applications, and to a novel process for synthesis of temozolomide esters by a direct esterification of temozolomide acid (3,4-dihydro-3-methyl-4-oxoimidazo[5,1-d]-1,2,3,5-tetrazine-8-carboxylic acid) with a halogeno-aliphatic compound in presence of a base, or with an alcohol in presence of a dehydrate agent
专利号:US-2025101006-A1 优先权日:2022-01-31 标题:Process for the synthesis of pyrazolyl derivatives useful as anti-cancer agents 发明人:BAENZIGER MARKUS; GALLOU FABRICE; GUO FENGFENG; HÄNGGI RUDOLF; HAN ENJIAN; JORDINE GUIDO; LI JIALIANG; LIU WEIPENG; MIAO BUKEYAN; RONG SHAOFENG; SANTANDREA ERNESTO; SCHIRNER PAUL BERND; SHEN XIAODONG; WANG CAN; ZHANG HAO 权利人:NOVARTIS AG 摘要:The invention provides a novel process, novel process steps and novel intermediates useful in the synthesis of pharmaceutically active compounds, especially KRAS G12C inhibitors. The present invention provides a direct enantioselective chemical manufacturing method of making Compound A, or a pharmaceutically acceptable hydrate or solvent thereof: (I). The invention provides a process for preparing Intermediate B6* comprising reacting Intermediate B4* with Intermediate B5* in an atroposelective coupling reaction, using a chiral catalyst.
专利号:US-9096647-B2 优先权日:2008-09-16 标题 :Simplified one-pot synthesis of [18F]SFB for radiolabeling 发明人:OLMA SEBASTIAN; SHEN CLIFTON KWANG-FU 权利人:UNIV CALIFORNIA 摘要:A non-aqueous single pot synthesis of [ 18 F]SFB is set forth. The [ 18 F]SFB produced with this method is then used, for example, to label a peptide or an engineered antibody fragment (diabody) targeting human epidermal growth factor receptor 2 (HER2) as representative examples of labeled compounds for use as an injectable composition to locate abnormal tissue, specifically tumors within an animal or human using a PET scan.
专利号:US-6069248-A 优先权日:1998-08-21 标题 :Process for the synthesis of triazolopyridazine compounds 发明人:BOLDI ARMEN M; JOHNSON CHARLES R 权利人:AXYS PHARM INC 摘要:The present invention provides a process for the synthesis of triazolopyridazine based compounds represented by Formula A: ##STR1## These compounds have utility as angiotensin related antihypertensive agents.
专利号:US-7279583-B2 优先权日:2003-12-10 标题:Process for the synthesis of perindopril and pharmaceutically acceptable salts thereof 发明人:DUBUFFET THIERRY; LECOUVE JEAN-PIERRE 权利人:SERVIER LAB 摘要:Process for the industrial synthesis of perindopril of formula (I): n nand pharmaceutically acceptable salts thereof.
参考文献:10.1007/s00216-012-6623-1 摘要:Rich RM, Stankowska DL, Maliwal BP, Sørensen TJ, Laursen BW, Krishnamoorthy RR, Gryczynski Z, Borejdo J, Gryczynski I, Fudala R. Elimination of autofluorescence background from fluorescence tissue images by use of time-gated detection and the AzaDiOxaTriAngulenium (ADOTA) fluorophore. Analytical and Bioanalytical Chemistry. 2012 Dec 20;405(6):2065–75. doi: 10.1007/s00216-012-6623-1.