CAS: 1893-33-0; 1'-(4-(4-Fluorophenyl)-4-Oxobutyl)-[1,4'-Bipiperidine]-4'-Carboxamide

上下游产品

(1,4’-二哌啶)-4’-甲酰胺 [1,4']Bipiperidinyl-4'-Carboxylic Acid Amide 39633-82-4
螺哌隆 Spiperone 749-02-0

1-(4-氯丁-1-炔-1-基)-4-氟苯置于水,碳酸氢钠,双三氟甲烷磺酰亚胺,Potassium Iodide体系中,用 1,4-二氧六环,甲苯 用作溶剂,化学反应生成酰胺哌啶酮
参考文献:Sonogashira反应与区域选择性水合反应合成相关药物化合物的邻/间/对位异构体
标题:Sonogashira反应与区域选择性水合反应合成相关药物化合物的邻/间/对位异构体
摘要:通过钯催化的sonogashira反应,然后在催化条件下,用三氟乙二酸或金催化剂将形成的炔烃进行区域选择性水合,制得邻位,间位和对位取代的芳基酮.该方法学为从容易获得的起始原料,卤代芳烃和末端炔烃中获得取代的芳基烷基酮开辟了道路.介绍了氟哌啶醇,美潘酮,哌帕酮和布洛芬的不同区域异构体的合成.通过多巴胺能和环氧合酶结合试验研究了这些化合物的结构活性关系.
Doi:10.1021/cs401075Z

专利信息

专利号:US-2012215002-A1
优先权日:2009-10-09
标 题:Synthesis of optically active intermediate for the preparation of montelukast
发明人：LEFORT LAURENT
权利人:LEFORT LAURENT
摘要:The present invention relates to the synthesis of optically active alcohols by means of enantioselective hydrogenation of ketones in biphasic systems. In particular the present invention relates to the synthesis of an optically active alcohol of general formula (1).

专利号:US-5877278-A
优先权日:1992-09-24
标题:Synthesis of N-substituted oligomers
发明人：ZUCKERMANN RONALD N; GOFF DANE A; NG SIMON; SPEAR KERRY; SCOTT BARBARA O; SIGMUND AARON C; GOLDSMITH RICHARD A; MARLOWE CHARLES K; PEI YAZHONG; RICHTER LUTZ; SIMON REYNA
权利人:CHIRON CORP
摘要:A solid-phase method for the synthesis of N-substituted oligomers, such as poly (N-substituted glycines) (referred to herein as poly NSGs) is used to obtain oligomers, such as poly NSGs of potential therapeutic interest which poly NSGs can have a wide variety of side-chain substituents. Each N-substituted glycine monomer is assembled from two 'sub-monomers' directly on the solid support. Each cycle of monomer addition consists of two steps: (1) acylation of a secondary amine bound to the support with an acylating agent comprising a leaving group capable of nucleophilic displacement by -NH2, such as a haloacetic acid, and (2) introduction of the side-chain by nucleophilic displacement of the leaving group, such as halogen (as a solid support-bound alpha -haloacetamide) with a sufficient amount of a second sub-monomer comprising an -NH2 group, such as a primary amine, alkoxyamine, semicarbazide, acyl hydrazide, carbazate or the like. Repetition of the two step cycle of acylation and displacement gives the desired oligomers. The efficient synthesis of a wide variety of oligomeric NSGs using automated synthesis technology of the present method makes these oligomers attractive candidates for the generation and rapid screening of diverse peptidomimetic libraries. The oligomers of the invention, such as N-substituted glycines (i.e. poly NSGs) disclosed here provide a new class of peptide-like compounds not found in nature, but which are synthetically accessible and have been shown to possess significant biological activity and proteolytic stability. Combinatorial libraries of cyclic compounds are disclosed wherein the cyclic compounds are comprised of at least one ring structure derived from cyclization of a peptoid backbone. The diversity of product compounds is generated by the sequential addition of substituted submonomers. The combinatorial library includes 10 or more, preferably 100 or more, and more preferably 1,000 or more distinct and different compounds. The library includes each of the product compounds in retrievable and analyzable amounts and preferably includes at least one biologically active compound. Methods of synthesizing the combinatorial libraries and assay devices produced using the libraries are disclosed as is methodology for screening for and obtaining biologically active cyclic organic compounds.

专利号:US-8138346-B2
优先权日:2006-08-16
标题 :Method for synthesis of 8-alkoxy-9H-isothiazolo[5,4-B]quinoline-3,4-diones
发明人：BRADBURY BARTON JAMES; WILES JASON ALLAN; HASHIMOTO AKIHIRO; WANG QIUPING; LUCIEN EDLAINE; PAIS GODWIN; KIM HA YOUNG
权利人:BRADBURY BARTON JAMES; WILES JASON ALLAN; HASHIMOTO AKIHIRO; WANG QIUPING; LUCIEN EDLAINE; PAIS GODWIN; KIM HA YOUNG; ACHILLION PHARMACEUTICALS INC
摘要:The present invention provides process for synthesis of 8-methoxy-9H-isothiazolo[5,4-b]quinoline-3,4-diones and 8A,9-dihydro-4aH-isothiazolo[5,4-b]quinoline-3,4-diones of the Formula A. n nThe substituents R, R 5 , R 6 , R 7 , R 8 and R 9 are defined herein. The invention also provides novel synthetic intermediates useful in the synthesis of 8-methoxy-9H-isothiazolo[5,4-b]quinoline-3,4-diones and 8A,9-dihydro-4aH-isothiazolo[5,4-b]quinoline-3,4-diones.

专利号:WO-0140193-A1
优先权日:1999-12-03
标题:Method for the synthesis of pyrazolines
发明人：BOLDI ARMEN M
权利人:CHEMRX ADVANCED TECHNOLOGIES I; BOLDI ARMEN M
摘要:The present invention provides a method for the synthesis of compounds of Formula (I). Also claimed are novel intermediates and their methods of synthesis.

专利号:US-2002103381-A1
优先权日:2000-11-30
标 题 :Method for the synthesis of pyrazolines
发明人：BOLDI ARMEN M
摘要:The present invention provides a method for the synthesis of compounds of Formula I: n n n Also claimed are novel intermediates and their methods of synthesis.

专利号:US-11999757-B2
优先权日:2017-11-01
标 题:Synthesis of boronate ester derivatives and uses thereof
发明人：BOYER SERGE HENRI; HECKER SCOTT J; VERZIJL GERARDUS K M; HERMSEN PETRUS J
权利人:MELINTA SUBSIDIARY CORP
摘要:Disclosed herein are methods for the preparation of boronate derivatives in the synthesis of antimicrobial compounds and uses thereof. Disclosed herein includes method of making a compound of Formula (B) by reducing the ketone group of the keto-ester compound of Formula (A), and the reduction can be performed using a Ruthenium based catalyst system or using an alcohol dehydrogenase bioreduction system.