专利号:US-5861532-A 优先权日:1997-03-04 标 题:Solid-phase synthesis of N-alkyl amides 发明人:BROWN EDWARD G; NUSS JOHN M 权利人:CHIRON CORP 摘要:Methods for solid phase synthesis of N-alkyl amides comprise reductive amination of carbonyl compounds using a reducing agent and an amine-containing linker bound to a solid support. The methods afford high yields of linker-bound, monoalkylated amines, and subsequent coupling with acid derivatives provide derivatized N-substituted amides in excellent yields after cleavage from the solid-phase. Compositions useful in solid phase synthesis are also described.
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-4592874-A 优先权日:1980-05-14 标 题:Process for the synthesis of alpha-chlorinated chloroformates 发明人:CAGNON GUY C; PITEAU MARC D; SENET JEAN-PIERRE G; OLOFSON ROY A; MARTZ JONATHAN T 权利人:POUDRES & EXPLOSIFS STE NALE 摘要:Process for the synthesis of alpha -chlorinated chloroformates, and new alpha -chlorinated chloroformates. The invention relates to a new process for the manufacture of alpha -chlorinated chloroformates and, to new alpha -chlorinated chloroformates as new industrial products. The process according to the invention consists of a synthesis, by catalytic phosgenation, of alpha -chlorinated chloroformates of the formula: in which: R represents a substituted or unsubstituted hydrocarbon radical and m represents an integer superior or equal to one, this synthesis consisting in reacting phosgene with the aldehyde R-CHO)m, in the presence of a catalyst which is an organic or inorganic substance which is capable in a medium containing an aldehyde of the formula R-CHO)m, phosgene and, possibly, a solvent, of generating a pair of ions one of which is an halogenide anion and the other is a cation which is sufficiently separated from said halogenide anion so as to give to the latter a nucleophilic power enabling it to react with the function(s) aldehyde of the molecule R-CHO)m.
专利号:US-2008146772-A1 优先权日:2006-11-02 标题 :Materials and methods for co-crystal controlled solid-state synthesis of imides and imines 发明人:ZAWOROTKO MICHAEL J; CHENEY MIRANDA L 权利人:UNIV SOUTH FLORIDA 摘要:The subject invention pertains to methods for solid-state synthesis of imides and imines using co-crystals. The co-crystal formers utilized are substrates of condensation reactions and co-crystals can be obtained in high yield via methods such as slurrying, solvent evaporation, solvent crystallization, treatment with supercritical fluid(s), melting plus crystallization, slurry conversion, grinding of solids, blending of powders, heating of solids, solvent-drop grinding, or grinding plus melting.
专利号:US-5763681-A 优先权日:1989-09-06 标 题 :Synthesis of stable, water-soluble chemiluminescent 1,2-dioxetanes and intermediates therefor 发明人:EDWARDS BROOKS; JUO RHOU-RONG 权利人:TROPIX INC 摘要:A novel synthesis of compound having the formula: ##STR1## wherein T is a stabilizing spiro-linked polycycloalkylidene group, R 3 is a C 1 -C 20 alkyl, aralkyl or heteroatom containing group, Y is an aromatic fluorescent chromophore, and Z is a cleavable group which, when cleaved, induces decomposition of the dioxetane ring and emission of optically detectable light, is disclosed. A tertiary phosphorous acid alkyl ester of the formula: n n (R.sup.1 O).sub.3 P n n wherein R 1 is a lower alkyl group, is reacted with an aryl dialkyl acetal produced by reacting a corresponding aryl aldehyde with an alcohol of the formula: n n R.sup.3 OH n n wherein R 3 is as defined above, to produce a 1-alkoxy-1-aryl-methane phosphonate ester of the formula: ##STR2## reacting the phosphonate with base to produce a phosphonate-stabilized carbanion, reacting the carbanion with a ketone of the formula: ##STR3## wherein T is as defined above, to produce an enol ether of the formula: ##STR4## then oxygenating the double bond in the enol ether to give the corresponding 1,2-dioxetane compound.
专利号:US-12209103-B2 优先权日:2018-06-22 标题:Nanoreactors for the synthesis of porous crystalline materials 发明人:PUIGMARTI-LUIS JOSEP; ZAMORA ABANADES FELIX JUAN; FRANCO PUJANTE CARLOS; RODRIGUEZ SAN MIGUEL DAVID; SORRENTI ALESSANDRO 权利人:UNIV MADRID AUTONOMA 摘要:The present invention relates to the field porous crystalline materials, more particularly to metal organic frameworks (MOFs) and covalent organic frameworks (COFs). According to this invention, micelles are used as nanoreactors for the synthesis and stabilisation of porous crystalline materials in aqueous dispersions. Disclosed are dispersions comprising such porous crystalline materials, the synthesis and use of such dispersions. Further disclosed are novel porous crystalline materials, the synthesis and use of such crystalline materials. Further disclosed are novel inks comprising the dispersions and non-solvent, the synthesis and use of such inks for direct printing, 2D printing and 3D printing.
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