7-氮杂吲哚置于硼烷四氢呋喃络合物,溴,溶剂黄146,锌体系中,用 四氢呋喃,水,叔丁醇 用作溶剂,化学反应生成5-溴-7-氮杂吲哚 参考文献:Application Of 7-Azaisatins In Enantioselective Morita-baylis-hillman Reaction 标题:Application Of 7-Azaisatins In Enantioselective Morita-baylis-hillman Reaction 摘要:7-氮杂异吲哚和7-氮杂氧吲哚骨架是多种生物活性物质中宝贵的构建模块.在这里,7-氮杂异吲哚在使用双功能三级胺β-异喹啉(β-Icd)作为催化剂与马来酰亚胺在恩曼选择性morita-baylis-hillman(mbh)反应中比类似的异吲哚更有效的亲电试剂.这条途径允许方便地获得高对映纯度(高达94% Ee)的多功能3-羟基-7-氮杂-2-氧吲哚.其他类型的活化烯烃,如丙烯酸酯和丙烯醛,也可以被有效利用. Doi:10.3762/bjoc.12.33
专利号:US-9994567-B2 优先权日:2015-05-22 标 题:Synthesis of heterocyclic compounds 发明人:IBRAHIM PRABHA N; LIN JACK; SPEVAK WAYNE; ZHANG JIAZHONG 权利人:PLEXXIKON INC 摘要:Provided herein are intermediates and processes useful for facile synthesis of compounds of formula (I): n nor a pharmaceutically acceptable salt, a solvate, a tautomer, an isomer or a deuterated analog thereof, wherein Q, P 1 and P 2 are as defined in this disclosure.
专利号:US-2006183758-A1 优先权日:2005-02-17 标 题:Method for synthesis of AZA-annelated pyrroles, thiophenes, and furans 发明人:BEARD CHARLES D; LEE VING J; WHITTLE C E 权利人:CB RES AND DEV INC 摘要:Methods of synthesis of intermediates that are useful as bioisosteres of the indole, benzofuran and benzothiophene scaffold are disclosed.
专利号:US-9695169-B2 优先权日:2012-05-31 标 题:Synthesis of heterocyclic compounds 发明人:IBRAHIM PRABHA N 权利人:PLEXXIKON INC 摘要:Provided herein are intermediates and processes useful for facile synthesis of biologically active molecules.
专利号:US-7652137-B2 优先权日:2003-03-06 标 题:Synthesis of 5 substituted 7-azaindoles and 7-azaindolines 发明人:GRACZYK PIOTR PAWEL; KHAN AFZAL; BHATIA GURPREET SINGH 权利人:EISAI R&D MAN CO LTD 摘要:The present invention provides a novel substituted azaindoline intermediate of formula (I) and a method for its synthesis. The novel substitued azaindoline intermediate (I) is provided for use in the manufacture of 5-substituted 7-azaindolines and 5-substituted 7-azaindoles.
专利号:US-2022073513-A1 优先权日:2018-12-29 标题:1h-pyrrolo[2,3-b]pyridine derivatives and related compounds as bcl-2 inhibitors for the treatment of neoplastic and autoimmune diseases 发明人:CHEN YI 权利人:NEWAVE PHARMACEUTICAL INC 摘要:The present invention relates to compounds of Formula (II) and more preferably to 1H-pyrrolo[2,3-b]pyridine derivatives of formula (III) and related compounds. The variables are defined in the claims. The compounds are BCL-2 inhibitors for treating neoplastic, autoimmune or neurodegenerative diseases. The present description discloses the synthesis of exemplary compounds as well as pharmacological data thereof (pages 61 to 72; examples 1 to 4; tables). An exemplary compound is e.g. 4-(4-[[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl]piperazin-1-yl)-2-[methyl(1H-pyrrolo[2,3-b]pyridin-5-yl)phosphoroso]-N-[3-nitro-4-[(oxan-4-yl methyl)amino]benzenesulfonyl]benzamide (example 1).
专利号:US-2018002332-A1 优先权日:2015-05-22 标题 :Synthesis of heterocyclic compounds