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-3781324-A 优先权日:1969-11-03 标 题:Certain 6-trifluoromethylcytosines and thiocytosines,their synthesis,and their use in the synthesis of uracils and thiouracils 发明人:LUTZ A 权利人:AMERICAN CYANAMID CO 摘要:3-AMINO-2-SUBSTITUTED - 4,4,4 - TRIFLUORO-2-BUTENENITRILES ARE REACTED WITH ISOCYANATES OR ISOTHIOCYANATES IN THE PRESENCE OF AN INERT SOLVENT AND FROM 0.75 TO ABOUT 1.0 MOLE EQUIVALENTS OF STRONG BASE PER MOLE OF BUTENENITRILE TO PRODUCE THE NOVEL UREIDO BUTENENITRILES OF THE FORMULA: CF3-C(-NH-C(=X)-NH-R)=C(-HALO)-CN WHEREIN R IS ALKYL, ALKENYL, PHENYL, BENZYL AND SUBSTITUTED DERIVATIVES THEREOF AND X IS SULFUR OR OXYGEN. THE UREIDO BUTENENITRILE ARE TREATED WITH ADDITIONAL BASE TO PRODUCE NOVEL CYCLIC CYTOSINES OF THE FORMULA: 6-CF3,5-HALO,4-(HN=),3-R,2-(X=)-1,2,3,4-TETRAHYDRO- PYRIMIDINE WHEREIN R AND X ARE AS DEFINED ABOVE. THE CYTOSINES CAN BE PRODUCED DIRECTLY BY TREATING 3-AMINO-2-SUBSTITUTED4,4,4-TRIFLUORO-2-BUTENENITRILE WITH AT LEAST 1.0 MOLE EQUIVALENT OF BASE. THE NOVEL COMPOUNDS ARE USEFUL INTERMEDIATES IN THE PREPARATION OF HERBICIDAL URACILS AND THIOURACILS.
专利号:US-9359327-B2 优先权日:2008-06-30 标题:Process for the preparation of substituted pyrimidine derivatives 发明人:CESCO-CANCIAN SERGIO; CHEN HONGFENG; GRIMM JEFFREY S; MANI NEELAKANDHA S; MAPES CHRISTOPHER M; PALMER DAVID C; PIPPEL DANIEL J; SORGI KIRK L; XIAO TONG 权利人:JANSSEN PHARMACEUTICA NV 摘要:The present invention is directed to processes for the preparation of substituted pyrimidine derivatives, useful as intermediates in the synthesis of histamine H 4 receptor modulators, and to intermediates in H4 modulator synthesis.
专利号:US-8252927-B2 优先权日:2008-07-22 标题:Synthesis of substituted 4-amino-pyrimidines 发明人:KARGE REINHARD; LETINOIS ULLA; SHIEFER GERHARD 权利人:KARGE REINHARD; LETINOIS ULLA; SHIEFER GERHARD; DSM IP ASSETS BV 摘要:The present invention is directed to a process for the manufacture of compounds of formula IV wherein R 1 is an amino protecting group, and R 2 is hydrogen or C 1-10 alkyl, comprising a) reacting a compound of formula Ia, wherein M + is a cation, preferably selected from the group consisting of Li + , Na+, K + , ½ Mg 2+ and ½ Zn 2+ , (formula 1 a ) with an ammonium salt NH 4 + X − , wherein X − is an anion, preferably selected from the group consisting of chloride, bromide, sulfate and acetate, in a solvent to a compound of formula II b) reacting a compound of formula II with a nitrile R 2 —CN in the presence of a base to a compound of formula IV. The present invention is further directed to compounds of formula II and their use for the manufacture of vitamin B 1 .
专利号:US-4686285-A 优先权日:1984-02-10 标题:Basic azo and non-azo compounds having one or two disubstituted 1,3,5-triazine rings each of which is linked through a bridging radical to the 1-position of a pyrazole ring 发明人:PEDRAZZI REINHARD 权利人:SANDOZ LTD 摘要:(i) Metal-free compounds of the formula ##STR1## (ii) tautomers thereof, (iii) 1:1 and 1:2 metal complexes of (i) and (ii), n (iv) salts of (i), (ii), and (iii), and n (v) mixtures of (i), (ii), (iii), and (iv), n wherein the symbols are as defined in the Specification, are useful as dyes for, for example, polymers and copolymers of acrylonitrile, polyesters modified to contain acid groups, polyamides such as wool, leather, cotton, bast fibers such as hemp, flax, sisal jute, coir and straw, regenerated cellulose, glass fibers and paper (those wherein R o is other than hydrogen) or as intermediates for the synthesis of dyes.
专利号:US-10226449-B2 优先权日:2013-12-20 标 题:Heterocyclic modulators of lipid synthesis and combinations thereof 发明人:HEUER TIMOTHY SEAN; OSLOB JOHAN D; MCDOWELL ROBERT S; JOHNSON RUSSELL; YANG HANBIAO; EVANCHIK MARC; ZAHARIA CRISTIANA A; CAI HAIYING; HU LILY W; DUKE GREGORY; OHOL-GUPTA YAMINI; O'FARRELL MARIE 权利人:3 V BIOSCIENCES INC 摘要:Heterocyclic modulators of lipid synthesis are provided as well as pharmaceutically acceptable salts thereof; pharmaceutical compositions comprising such compounds; and methods of treating conditions characterized by dysregulation of a fatty acid synthase pathway by the administration of such compounds and combinations of such compounds and other therapeutic agents.
[参考文献]: Elena I Klimova, Et Al. 4-Ferrocenylpyridine- And 4-Ferrocenyl-3-Ferrocenylmethyl-3,4-Dihydropyridine-3,5-Dicarbonitriles: Multi-Component Synthesis, Structures And Electrochemistry. Molecules. 2012 Aug 24;17(9):10079-93.
合成参考文献
摘要:Sainsbury, M., Science of Synthesis Knowledge Updates, (2010) 1, 225. 摘要:von Angerer, S., Science of Synthesis Knowledge Updates, (2011) 1, 234.