专利号:US-9193691-B2 优先权日:2012-04-27 标题:Methods for the synthesis of activated ethylfumarates and their use as intermediates 发明人:KRAFT KELLY SULLIVAN; FREEMAN JOHN J; SERWINSKI PAUL; PAVIA VINNIE; PHANSTIEL OTTO; KAUR NAVNEET 权利人:MANNKIND CORP; MANNKIND CORP 摘要:Disclosed embodiments relate to improved methods for the synthesis of activated fumarate intermediates and their use in chemical synthesis. Disclosed embodiments describe the synthesis of activated fumarate esters including those derived from activating groups including: 4-nitrophenyl, diphenylphosphoryl azide, pivaloyl chloride, chlorosulfonyl isocyanate, p-nitrophenol, MEF, trifluoroacetyl and chlorine, for example, ethyl fumaroyl chloride and the subsequent use of the activated ester in situ. Further embodiments describe the improved synthesis of substituted aminoalkyl-diketopiperazines from unisolated and unpurified intermediates allowing for improved yields and reactor throughput.
专利号:WO-2004037772-A1 优先权日:2002-10-22 标 题 :Convenient and scalable synthesis of ethyl n-[(2-boc-amino) ethyl] glycinate and its hydrochloride salt 发明人:HUDSON ROBERT H E; VIIRRE RUSSELL D 权利人:UNIV WESTERN ONTARIO; HUDSON ROBERT H E; VIIRRE RUSSELL D 摘要:The present invention discloses an improved synthesis of ethyl N-[(2-Boc-amino)ethyl]glycinate and its hydrochloride salt. The synthesis is based on the reductive alkylation of Boc-ethylenediamine with ethyl glyoxylate hydrate and furnishes the title compound in near quantitative yield and high purity without chromatography. This compound is suitable, as is, for the synthesis peptide nucleic acid monomers. Further, conversion to the hydrochloride salt provides a stable, non-hygroscopic solid that is a convenient form for handling and storage.
专利号:US-8273887-B2 优先权日:2008-09-30 标题:Processes for synthesis of opiate alkaloid derivatives 发明人:MANNINO ANTHONY; ZDRODOWSKI JAMES 权利人:MANNINO ANTHONY; ZDRODOWSKI JAMES; MALLINCKRODT LLC 摘要:The present invention provides processes for the synthesis of opiate alkaloids. In particular, the opiate alkaloids produced by the process of the invention are typically intermediate compounds that may be utilized to produce a variety of biologically active alkaloids including buprenorphine and diprenorphine.
专利号:US-6509506-B1 优先权日:1997-05-21 标 题 :Two step synthesis of D- and L- α-amino acids and D- and L- α-amino aldehydes 发明人:SHARPLESS K BARRY; LI GUIGEN 权利人:SCRIPPS RESEARCH INST 摘要:D- and L- α-amino acids and D- and L-α-amino aldehydes are synthesized from olefin substrates in two steps. The first step is a catalyzed asymmetric aminohydroxylation addition reaction to the olefin substrate. The addition reaction is catalyzed by osmium and is co-catalyzed by chiral ligands. The chiral ligands, in addition to being co-catalysts with the osmium, also serve to direct the addition reaction regioselectively and enantioselectively, divalent ligands are preferred over monovalent ligands because of their enhanced regio-and enantio-selectivity. As an oxidant nitrogen source for the addition reaction, either a carbamate or sulfonamide may be employed. If carbamate is employed as an oxidant nitrogen source, the resultant β-hydoxycarbamate is deprotected to yield the corresponding β-hydroxyamine. If sulfonamide is employed as an oxidant nitrogen source, the resultant β-hydroxysulfonamide is deprotected to yield the corresponding β-hydroxyamine. The resultant β-hydroxyamine is then selectively oxidized in a second synthetic step to produce the desired D- and L- α-amino acid or D- and L-α-amino aldehyde.
专利号:US-9365874-B2 优先权日:2007-08-10 标 题 :Methods for synthesis of olefins and derivatives 发明人:BURK MARK J; PHARKYA PRITI; VAN DIEN STEPHEN J; BURGARD ANTHONY P; SCHILLING CHRISTOPHE H 权利人:GENOMATICA INC 摘要:The invention provides a method of producing acrylic acid. The method includes contacting fumaric acid with a sufficient amount of ethylene in the presence of a cross-metathesis transformation catalyst to produce about two moles of acrylic acid per mole of fumaric acid. Also provided is an acrylate ester. The method includes contacting fumarate diester with a sufficient amount of ethylene in the presence of a cross-metathesis transformation catalyst to produce about two moles of acrylate ester per mole of fumarate diester. An integrated process for process for producing acrylic acid or acrylate ester is provided which couples bioproduction of fumaric acid with metathesis transformation. An acrylic acid and an acrylate ester production also is provided.
专利号:US-7417142-B2 优先权日:2002-03-28 标 题:Chiral porphyrins, chiral metalloporphyrins, and methods for synthesis of the same 发明人:ZHANG X PETER; CHEN YING; GAO GUANG-YAO 权利人:UNIV TENNESSEE RES FOUNDATION 摘要:Novel methods of synthesizing heteroatom-containing chiral porphyrins and chiral metalloporphyrins and the novel chiral porphyrins and chiral metalloporphyrins themselves are disclosed. Metal complexes of the chiral porphyrins are prepared in high yields and shown to be active catalysts for highly enantioselective and diastereoselective cyclopropanation, aziridination, and epoxidation of alkenes under a practical one-pot protocol.
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合成参考文献
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