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(1-苄基哌啶-4-基)(甲基)氨基甲酸叔丁酯 1-Benzyl-4-[n-(Tert-Butoxycarbonyl)Methylamino]Piperidine 139062-92-3
4-(N-叔丁氧羰基-N-甲基氨基)哌啶-1-羧酸苄酯 Benzyl 4-((Tert-Butoxycarbonyl)(Methyl)Amino)Piperidine-1-Carboxylate 405057-76-3
1-苄基-4-(Boc-氨基)哌啶 Tert-Butyl (1-Benzylpiperidin-4-yl)Carbamate 73889-19-71-苄基-4-甲氨基哌啶置于palladium 10% On Activated Carbon,氢气,三乙胺体系中,用 甲醇,二氯甲烷 用作溶剂,化学反应 72.0H,反应生成4-N-叔丁氧羰基-4-N-甲基氨基哌啶
参考文献:从杂芳基氯化物有效钯催化合成1-杂芳基-4-氨基哌啶衍生物
标题:从杂芳基氯化物有效钯催化合成1-杂芳基-4-氨基哌啶衍生物
摘要:描述了一种从杂芳基氯衍生物开始合成1-杂芳基-4-(n-甲基)氨基哌啶的有效方案.使用davephos作为pd催化的buchwald-Hartwig胺化反应的最佳配体,可以以非常好或优异的收率获得多种1-杂芳基-4-(n-Boc-N-甲基)氨基哌啶衍生物.经过温和有效的酸解后,可以成功获得胺化产物.
Doi:10.1016/j.Tetlet.2017.04.014
专利信息
专利号:US-5420283-A
优先权日:1993-08-02
标 题 :Resolution of (R)-2-benzylsuccinic acid 4-[4-(N-t-butoxycarbonylmethylamino)-piperidine] amide
发明人:DUGGER ROBERT W
权利人:PFIZER
摘要:This invention relates to with a novel synthesis of (R)-2-benzylsuccinic acid 4-[4-(N-t-butoxycarbonyl-methylamino)-piperidine]amide from racemic intermediates. The racemic (R)-2-benzylsuccinic acid 4-[4-(N-t-butoxycarbonyl-methylamino)piperidine]amine is resolved through the formation of diasteromic salts with (S)-cyclohexylethylamine or (R)-cyclohexylethylamine. The pure diasteromic salt can be subsequently hydrolyzed with dilute acid to yield the pure enantiomer of (R)-2-benzylsuccinic acid 4-[4-(N-t-butoxycarbonyl-methylamino) piperidine]amide.
专利号:US-12150934-B2
优先权日:2016-11-30
标 题 :Methods of using substituted pyrazole and pyrazole compounds and for treatment of hyperproliferative diseases
发明人:SIDDIQUI ARSHAD M; CIBLAT STEPHANE; CONSTANTINEAU-FORGET LEA; GRAND-MAITRE CHANTAL; GUO XIANGYU; SRIVASTAVA SANJAY; SHIPPS GERALD W; COOPER ALAN B; OZA VIBHA; KOSTURA MATTHEW W; LUTHER MICHAEL; LEVINE JEDD
权利人:BANTAM PHARMACEUTICAL LLC
摘要:Disclosed are methods of treating hyperproliferative disorders such as cancer, methods of arresting the cell cycle in cancer cells, methods of inhibiting glutathione synthesis in cancer cells, and associated compounds for use and uses in medicaments. In certain embodiments, the methods, uses and compounds are provided with reference to compounds of the structural formula (I), in which X1, X2, Z1, Z2, the ring system denoted by “aâ€?, R1, L1, L2, Q, L3, R3, L4, R4, L5, and R5 are as described herein. In certain embodiments, compounds disclosed herein are especially active against cancers having a mutant KRAS gene.
专利号:US-12018014-B2
优先权日:2018-09-19
标题:Pyrrole-substituted indolone derivative or pharmaceutically acceptable salts thereof, and preparation method therefor and application thereof
发明人:HU LIHONG
权利人:SUZHOU GENHOUSE PHARMACEUTICAL CO LTD; SHANDONG NEW TIME PHARMACEUTICAL CO LTD
摘要:A pyrrole-substituted indolone derivative or pharmaceutically acceptable salts thereof, and a preparation method therefor and application thereof. The pyrrole-substituted indolone derivative or pharmaceutically acceptable salts thereof is simple to synthesize, easy to prepare, rich in raw materials for synthesis, and has an inhibitory effect on a plurality of tyrosine kinases, especially has higher selective inhibitory activity against KDR (VEGFR2), and FLT3 and its mutants, and can avoid toxic side effects caused by inhibiting KDR.
专利号:CN-114249680-B
优先权日:2022-01-10
标 题:A kind of indole derivative and its synthesis method and application
专利号:US-11286268-B1
优先权日:2019-07-02
标题:EIF4E-inhibiting compounds and methods
发明人:SPERRY SAMUEL; XIANG ALAN X; ERNST JUSTIN T; REICH SIEGFRIED H; SPRENGELER PAUL A; SHAGHAFI MIKE; MICHELS THEO; NILEWSKI CHRISTIAN; TRAN CHINH VIET; PACKARD Garrick Kenneth; GRUBBS ALAN; URKALAN KAVERI; MUKAIYAMA TAKASUKE
权利人:EFFECTOR THERAPEUTICS INC
摘要:The present invention provides synthesis, pharmaceutically acceptable formulations and uses of compounds in accordance with Formula I, or a stereoisomer, tautomer or pharmaceutically acceptable salt thereof. n n n n n n n n n n For Formula I compounds X 1 , X 2 , X 3 , X 4 , X 5 , X 6 , Q, L 1 , L 2 , Y, R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 8 and rings A, B and C are as defined in the specification. The inventive Formula I compounds are inhibitors of eIF4e and find utility in any number of therapeutic applications, including but not limited to treatment of inflammation and various cancers.