专利号:US-6177564-B1 优先权日:1998-09-11 标题:Process for the synthesis of N-benzyl-3-(4-fluorophenyl)-1-4-oxazin-2-one 发明人:NELSON TODD D; BHUPATHY MAHADEVAN 权利人:MERCK & CO INC 摘要:The present invention is concerned with a novel process for the preparation of N-benzyl-3-(4-fluorophenyl)-1,4-oxazin-2-one of the formula:This compound is useful as an intermediate in the synthesis of compounds which possess pharmacological activity, in particular, as substance P (neurokinin-1) receptor antagonists.
专利号:WO-2025108921-A1 优先权日:2023-11-22 标 题 :Synthesis of radiopharmaceutical agents 发明人:AUZELOUX PHILIPPE; LEVESQUE SOPHIE; GALMIER MARIE-JOSÈPHE; CHEZAL JEAN-MICHEL 权利人:INST NAT SANTE RECH MED; UNIV CLERMONT AUVERGNE; CENTRE LUTTE CONTRE LE CANCER 摘要:Synthesis of radiopharmaceutical agents It is disclosed a method to synthesize a compound of formula (I), or a pharmaceutically acceptable salt thereof: Formula (I), (I) said process comprising contacting a trialkylstannane precursor of formula (II), or a pharmaceutically acceptable salt thereof: Formula (II), (II) with an alkali metal salt of a radionuclide selected from the group consisting of 123I, 124I, 125I, 131I, 211At, in appropriate acidic conditions and in presence of a peroxide ROOH in an 10 appropriate concentration. Said method is particularly suited for synthesizing [131I]N-(2- diethylaminoethyl)-6-iodoquinoxaline-2-carboxamide, providing a notable reduction in the quantity of side products, allowing a much purer finished product, while making use of reagents which are adapted to the constraints which need to be met when developing a product for clinical use and, more in particular, to the constraints to be met in order to 15 adapt the process for being fully automated.
专利号:WO-2024157132-A1 优先权日:2023-01-25 标 题 :Process for the preparation of an intermediate useful for the synthesis of voclosporin 发明人:ROSITANO VINCENZO; MOLINARI MARCO; SENALDI LUCA; ALLEGRINI PIETRO 权利人:INDENA SPA 摘要:The invention relates to a process for the preparation of an intermediate useful for the synthesis of voclosporin, an immunosuppressant active ingredient inhibitor of calcineurin.
专利号:US-10173993-B2 优先权日:2015-12-09 标题 :Process for the synthesis of sulfones and sulfonamides 发明人:VON WOLFF NIKLAS; CHAR JOËLLE; CANTAT THIBAULT 权利人:COMMISSARIAT ENERGIE ATOMIQUE 摘要:A one pot single step process is described for the synthesis of a compound, including a labeled compound, containing a sulfonyl functional group comprising the step of mixing together a silane, an SO 2 source, an electrophilic compound, an activating compound and optionally a metal catalyst. A process for producing tracers from a labeled sulfonyl containing compound prepared by the described process is also included.
专利号:US-6818773-B2 优先权日:2001-10-15 标题:Synthesis of 4-[(Z)-4-bromophenyl)(ethoxyimino) methyl]-1'-[(2,4-dimethyl-1-oxido-3-pyridinyl)carbony)]-4'-methyl-1,4-′bipiperidine 发明人:CHEN MINZHANG; D SA BOSCO ANTHONY; LEONG WILLIAM W; GAN TONG; WONG GEORGE S K; TANG SUHAN; NIELSEN CHRISTOPHER MICHAEL 权利人:SCHERING CORP 摘要:In one embodiment, the present invention describes the synthesis of 4-[(Z)-(4-bromophenyl)(ethoxyimino)methyl]-1'-[(2,4-dimethyl-1-oxido-3-pyridinyl)carbonyl]-4'-methyl-1,4'-bipiperidine, and intermediates therefor from easily available starting materials by a simple route.
专利号:WO-2007094746-A1 优先权日:2006-02-16 标 题 :5,7-dimethyladamantane-1,3-dicarboxylic acid dialkyl esters, a method for the synthesis thereof and method for synthesising a 5,7-dimethyladamantane-1,3-dicarboxylic acid in the form of an intermediate product 发明人:GOLOVKO LEONID VLADIMIROVICH; PILJAVSKY VOLODIMIR STEPANOVIC; BOYKO OLEKSANDR POLIKARPOVICH; KHILCHEVSKYY OLEKSANDR MIKOLAY; PETRENKO OLEKSANDR EVGRAFOVICH 权利人:GOLOVKO LEONID VLADIMIROVICH; PILJAVSKY VOLODIMIR STEPANOVIC; BOYKO OLEKSANDR POLIKARPOVICH; KHILCHEVSKYY OLEKSANDR MIKOLAY; PETRENKO OLEKSANDR EVGRAFOVICH 摘要:5,7-dimethyladamantane-1,3-dicarboxylic acid dialkyl esters of general formula (I), wherein R is C4 - C30 alkyl. Method for synthesis of said dialkyl esters consists in synthesising 5,7- dimethyladamantane-1,3-dicarboxylic acid chloride, alcoholising said chloride by aliphatic alcohol in a boiling benzene or toluene, removing a solvent and in purifying a target product. Method for synthesising 5,7-dimethyladamantane-1,3-dicarboxylic acid in the form of an intermediate product consists in synthesising perhydroacenaphthene by acenaphthene hydrogenation, isomerizating perhydroacenaphthene into 1,3-dimethyladamantane in the presence of AICI3, in synthesising 1,3-dimethyl-5,7-dibromoadamantane by two- stage bromation of 1,3-dimethyladamantane in such a way that a monobromoderivative thereof is obtained at the first stage, is subsequently converting it into 1,3-dimethyl-5,7-dibromoadamantane at the second stage and in carboxylating said compound by formic acid in the presence of 10-20% oleum.
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