CAS: 50-55-5; Reserpine

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CAS号482-98-4 Yohimban-16-met...

Dimethyl (3As,4S,6R,7S,7As)-6-[tert-Butyl(Dimethyl)Silyl]Oxy-2-Hydroxy-7-Methoxy-3,3A,4,5,6,7-Hexahydro-2H-1-Benzofuran-4,7A-Dicarboxylate置于2,6-二甲基吡啶,4-二甲氨基吡啶,Samarium Diiodide,硼烷四氢呋喃络合物,氢氟酸,乙二醇,三乙胺,三甲基乙酸体系中,用 四氢呋喃,六甲基磷酰三胺,二氯甲烷,甲苯,乙腈,苯 作为反应溶剂,化学反应 21.67H,反应生成 利血平
参考文献:使用chiron方法的(-)-利血平全合成.
标题:使用chiron方法的(-)-利血平全合成.
摘要:从(-)-奎宁酸作为手性模板开始,已开发了立体立体控制的利血平环d / E前体的合成方法.(-)-利血平的总合成通过内酰胺铵中间体的环化来描述.
DOI:10.1021/jo961713W

专利信息

专利号:WO-2010103857-A1
优先权日:2009-03-12
标 题 :Method for solid-phase synthesis of glycopeptide using silicon-containing protecting group and synthesis device
发明人：NISHIMURA SHIN-ICHIRO; SHIMAWAKI KEN
权利人:UNIV HOKKAIDO NAT UNIV CORP; NISHIMURA SHIN-ICHIRO; SHIMAWAKI KEN
摘要:Disclosed are a novel method for the synthesis of a glycopeptide by which glycopeptides of various types can be deprotected and excised from a resin, each under weakly acidic to weakly basic conditions, without causing the problems of the epimerization of an amino acid at the a-position and the ß-elimination of a sugar residue; a synthesis device therefor; and a synthesis intermediate to be used in synthesizing a glycopeptide. Specifically disclosed are a method for the solid-phase synthesis of a glycopeptide which comprises a step for obtaining a glycopeptide derivative wherein the N-terminus is protected, the C-terminus is immobilized to a solid phase via a silicon linker, and a reactive group carried by a sugar residue and a reactive group carried by an amino acid side chain constituting a peptide are protected by silicon-containing groups, and a step for obtaining the glycopeptide by deprotecting said glycopeptide derivative and releasing the same from the solid phase by treating the glycopeptide derivative with an agent for removing the silicon-containing groups and the silicon linker; a synthesis intermediate to be used in the step for obtaining the glycopeptide derivative in the aforesaid method; and a device for the solid-phase synthesis of a glycopeptide.

专利号:WO-0206209-A1
优先权日:2000-07-19
标 题 :Synthesis method for n1,n3-bis (2.aminoethyl) propane-1,3-diamine, synthesis intermediates, resulting products and use thereof in synthesis of cyclam
发明人：HANDEL HENRI; BERNARD HELENE; ANTOINE MARINE
权利人:UNIV BRETAGNE OCCIDENTALE; HANDEL HENRI; BERNARD HELENE; ANTOINE MARINE
摘要:The invention concerns a method of synthesis of a linear polynitrogen-containing derivative, namely N1,N3-bis (2-aminoethyl) propane-1,3-diamine of general formula (I) using as synthesis intermediates compounds (II) and (III). The invention also concerns the resulting products and their use in the synthesis of cyclic polynitrogen-containing derivatives such as cyclam.

专利号:WO-9837078-A1
优先权日:1997-02-20
标题 :Solid phase and combinatorial synthesis of substituted thiophenes and of arrays of substituted thiophenes
发明人：DOERWALD FLORENCIO ZARAGOZA
权利人:NOVO NORDISK AS
摘要:A solid phase method for the synthesis of a plurality of differently substituted thiophenes with a wide variety of side-chain substituents as compounds of potential therapeutic interest. The thiophenes are prepared by reaction of a substrate-bound primary or secondary amine with a thiophosgene equivalent and reaction of the resulting intermediate with an acceptor-substituted acetonitrile in the presence of a base. Alkylation with an appropriate alkyl halide, followed by Thorpe-Ziegler-cyclization yields differently substituted, support-bound 3-aminothiophenes. These may be screened on the substrate or cleaved from the substrate and then screened in solution. Alternatively, the resin-bound 3-amino thiophenes or the synthetic intermediates can be subjected to further synthetic transformations (N-acylation, reduction) on the support, which permits the preparation of further therapeutically interesting compounds. The efficient synthesis of a wide variety of thiophenes using automated synthesis technology of the present method makes these compounds attractive candidates for the generation and rapid screening of diverse thiophene-based libraries. The method disclosed here provides an easy and fast access to highly diverse heterocyclic compounds of therapeutic interest, amenable to automatization.

专利号:WO-2023012709-A1
优先权日:2021-08-05
标 题 :An improved process for fmoc synthesis of semaglutide
发明人：LOBO LESTER JOHN; CHANDRAKESAN MURALIDHARAN; DOSHI CHETAN; CHANADAK SHAILESH LALCHAND; YADAV NANDLAL GOPAL; MOHE NIKHIL UMESH; VISHWANATHAN KODANDARAMAN
权利人:USV PRIVATE LTD
摘要:The present invention relates to an improved process for the synthesis of glucagon-like-peptide-1 (GLP-1) and its analogs by using combination of solid and solution phase synthesis of Fmoc protected amino acids in a sequential manner, optionally incorporating Boc protected dipeptide for unnatural amino acid in the Sequence of GLP-1, cleaving GLP-1 sequence from the resin followed by purification; attaching side-chain to the desired amino acid in the solution phase to synthesize desired GLP-1 analog, purifying it to Semaglutide. Temperature gradient is applied during initial coupling of amino acids to facilitate completion of difficult coupling reactions.

专利号:US-7294486-B2
优先权日:2001-09-05
标 题:Enzymatic process for the synthesis of organo-fluorine compounds
发明人：O'HAGAN DAVID; SCHAFFRATH CHRISTOPH
权利人:UNIV ST ANDREWS
摘要:There is described a process for the synthesis of a fluoronucleoside compound, said process comprising mixing a substrate and an enzyme from Streptomyces cattelya as catalyst. The process may be used to produce an 18 F labelled fluoronucleoside compound. There is also described an enzyme derived from Streptomyces cattelya which has the capacity to catalyse the synthesis of a fluoronucleoside compound.

专利号:US-2004138469-A1
优先权日:2002-12-23
标 题 :Process for the synthesis of torsemide, in particular of pure and stable form II
发明人：LUSSANA MASSIMILIANO; RAINONI MAURO; GAMBUZZA FILIPPO
权利人:COSMA S P A
摘要:The present invention relates to a new process for the synthesis of torsemide, in particular of pure and stable form II, which comprises direct synthesis of torsemide from 4-(3-methylphenylamino)-3-pyridine-sulphonamide. The new process envisages fewer steps than the processes described in the prior art, with improved yields and good quality from the chemical and preferably polymorphous points of view.