Oxalate Salt Of 3-[2-(Dimethylamino)Ethyl]-N-Ethoxycarbonyl-N-Methyl-1H-Indole-5-Methanesulphonamide置于甲醇,氢氧化钾体系中,用 水 用作溶剂,化学反应 5.0H,以95%的收率获得磺马曲坦 参考文献:Synthesis Of 5-Substituted Indole Derivatives,I. An Improved Method For The Synthesis Of Sumatriptan 标题:Synthesis Of 5-Substituted Indole Derivatives,I. An Improved Method For The Synthesis Of Sumatriptan 摘要:An Improved Synthesis Of Sumatriptan (Ib) Via Fischer Cyclization Was Achieved By Introducing The Ethoxycarbonyl Group On The N-Atom Of The Sulphonamide Moiety In N-Methyl-4-Hydrazinobenzenemethanesulphonamide (7). As A Result,Substitution On The Benzylic Carbon Of The Indole Nucleus Could Be Avoided; However,Formation Of 1,1-Bis-(Indol-2-yl)-4-Dimethylaminobutane-Type By-Product (19) Was Observed. The Indolization Procedure Was Optimized To Suppress The Unwanted Side Reaction. The N-Protection Of The Sulphonamide Moiety Was Found To Be Beneficial Regarding The Purification Of The 3-[2-(Dimethylamino)Ethyl]-N-Ethoxycarbonyl-N-Methyl-1H-Indole-5-Methanesulphonamide (18). Doi:10.3987/com-97-8087
专利信息
专利号:US-8822702-B2 优先权日:2002-12-20 标 题 :Synthesis of amines and intermediates for the synthesis thereof 发明人:BERENS ULRICH; DOSENBACH OLIVER; SPRENGER DANIEL 权利人:BERENS ULRICH; DOSENBACH OLIVER; SPRENGER DANIEL; BASF SE 摘要:The invention relates in a first embodiment to a method for the manufacture of esters of the formula I, n nor especially of amides of the formula II,n n nwherein the symbols have the meanings given in the specification, as well as other intermediates and compounds useful in the synthesis of tryptamines and other substances mentioned in the title. The synthesis methods and intermediates are useful in the synthesis of pharmaceuticals.
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-2025188502-A1 优先权日:2022-03-10 标 题 :Biocatalyst and method for the synthesis of ubrogepant intermediates 发明人:CHEN HAIBIN; HU HU; CAI BAOQIN; XU JUNPENG; LIU SITONG; JIN LUPING; WU XINWEI; CUI QINYAN; ZHANG CHENGXIAO; ZHU KAILONG 权利人:ENZYMASTER NINGBO BIO ENG CO LTD 摘要:This application provides engineered transaminase polypeptides for the synthesis of Ubrogepant intermediates with high stereoselectivity, high catalytic activity and good stability. This application also provides a reaction process for the asymmetric synthesis of Ubrogepant intermediates using the transaminase polypeptide.
专利号:US-8697876-B2 优先权日:2010-04-02 标 题:Compositions and methods of synthesis of pyridinolypiperidine 5-HT1F agonists 发明人:CARNIAUX JEAN-FRANCOIS; CUMMINS JONATHAN 权利人:CARNIAUX JEAN-FRANCOIS; CUMMINS JONATHAN; COLUCID PHARMACEUTICALS INC 摘要:The present invention provides a novel polymorph of the hemisuccinate salt of 2,4,6-trifluoro-N-[6-(1-methyl-piperidine-4-carbonyl)-pyridin-2-yl]-benzamide (Form A) characterized by a unique X-ray diffraction pattern and Differential Scanning Calorimetry profile, as well as a unique crystalline structure. This polymorph is useful in pharmaceutical compositions, for example, for the treatment and prevention of migraine. The invention also provides a process for the synthesis of pyridinoylpiperidine compounds of Formula I in high yield and high purity. In particular, the provides a process for the preparation of 2,4,6-trifluoro-N-[6-(1-methyl-piperidine-4-carbonyl)-pyridin-2-yl]-benzamide, its hemisuccinate salt and polymorph (Form A).
专利号:US-7786156-B2 优先权日:2004-01-28 标 题 :Synthesis methods and intermediates for the manufacture of Rizatriptan 发明人:MARTIN PIERRE; BERENS ULRICH; BOUDIER ANDREAS; DOSENBACH OLIVER 权利人:RATIOPHARM GMBH 摘要:The invention relates to a process for the manufacture of an 1,2,4-triazol-1-yl compound of the formula [A], n nor a salt thereof, wherein each of R3 and R4 is hydrogen or lower alkyl, said process comprising reacting a hydrazine compound of the formula [B]n n nwherein R is hydrogen or acyl, R2 is hydrogen or a protecting group, are hydrogen or lower alkyl, and R6 is hydrogen or COOR7, or a salt thereof, with a 1,2,4-triazolyl forming reagent.n n In addition, novel intermediates for the synthesis of the anti-migraine agent Rizatriptan and methods for their synthesis are presented.
专利号:US-2024082118-A1 优先权日:2021-05-19 标 题:Topical compositions and methods of preparing the same 发明人:ABRAMOVICH SAGI; AVIDOR GAL; LANDA BENZION 权利人:LANDA LABS 2012 LTD 摘要:There is disclosed a composition comprising a water-insoluble thermoplastic compound capable of stimulating collagen synthesis (CSSC), the CSSC having a molecular weight of more than 0.6 kDa and being dispersed in a polar carrier as nano-elements having an average diameter of 200 nm or less and a viscosity of 107 mPa·s or less. The nano-elements of CSSC can be capable of stimulating the synthesis of skin proteins and/or enabling the delivery of active agents upon their application to a surface to be treated therewith. Methods for preparing the compositions and uses thereof are also provided.
1: Tajti J, Csáti A, Szok D. Szumatriptán–naproxén-nátrium fix dózisú kombinációja a migrén akut kezelésében – irodalmi áttekintés [Sumatriptan- naproxen sodium fix-dose combination for acute migraine treatment, a review]. Ideggyogy Sz. 2023 Sep 30;76(9-10):293-296. Hungarian. doi: 10.18071/isz.76.0293. 142:68-75. doi: 10.1016/j.pediatrneurol.2023.01.016. Epub 2023 Feb 4. 12(4):102-116. doi: 10.4103/jwas.jwas_183_22. Epub 2022 Nov 23. 4: Assadpour S, Shiran MR, Asadi P, Akhtari J, Sahebkar A. Harnessing Intranasal Delivery Systems of Sumatriptan for the Treatment of Migraine. Biomed Res Int. 2022 Jan 15;2022:3692065. doi: 10.1155/2022/3692065.
合成参考文献
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