CAS: 3647-74-3; 3A,4,7,7A-Tetrahydro-1H-4,7-Methanoisoindole-1,3(2H)-Dione

上下游产品

CAS号826-62-0 NA-酸酐 | CAS号74-89-5 氨基甲烷

纳迪克酸酐置于氯化胆碱,尿素体系中,化学反应 1.0H,以86%的收率获得产物5-降冰片烯-2,3-二甲酰亚胺
参考文献:在低共熔溶剂(des)氯化胆碱/脲中由酸酐和尿素合成n-未取代的环酰亚胺
标题:在低共熔溶剂(des)氯化胆碱/脲中由酸酐和尿素合成n-未取代的环酰亚胺
摘要:N-未取代的环状酰亚胺很容易在深共熔溶剂(des)胆碱氯化物(chcl)/脲中由具有尿素的酸酐合成.尿素既是des组分又是氮源,这使该方案具有反应平稳,产物易于分离,Chcl /脲易于回收和再循环的优点.
DOI:10.1007/s11696-019-00969-6

专利信息

专利号:US-4704450-A
优先权日:1983-02-21
标 题 :Synthesis of hpGRF(Somatocrinin) in liquid phase and intermediate peptides
发明人：DIAZ JOSEPH; DEMARNE HENRI; RONCUCCI ROMEO; SCHMELCK PAUL-HENRY
权利人:SANOFI SA
摘要:The invention relates to synthesis of hpGRF (Somatocrinin) in liquid phase and to intermediate peptides, comprising: coupling, one after the other and in the order of the sequence of the GRF, the fragments in which: (a) the side acid functions of the aspartic and glutamic acids and the side amine function of the lysine are protected by protector groups stable in the conditions of deprotection of the group Boc, (b) the guanidine function of the arginine is protected by protonation, and (c) the N-terminal amino acid is protected on the amine by the Boc group; selectively eliminating the group Boc from the N-terminal amine of the peptide in phase of elongation by hydrolysis with trifluoroacetic acid, said coupling being effected in an aprotic polar solvent and eliminating, at the end of sequence, all the protector groups by hydrolysis with the aid of a 0.1 to 1M solution of methanesulfonic or trifluoromethanesulfonic acid in trifluoroacetic acid.

专利号:US-4581168-A
优先权日:1983-02-21
标题:Synthesis of hpGRF (Somatocrinin) in liquid phase and intermediate peptides
发明人：DIAZ JOSEPH; DEMARNE HENRI; RONCUCCI ROMEO; SCHMELCK PAUL-HENRY
权利人:SANOFI SA
摘要:The invention relates to synthesis of hpGRF (Somatocrinin) in liquid phase and to intermediate peptides, comprising:--coupling, one after the other and in the order of the sequence of the GRF, the fragments in which: (a) the side acid functions of the aspartic and glutamic acids and the side amine function of the lysine are protected by protector groups stable in the conditions of deprotection of the group Boc, (b) the guanidine function of the arginine is protected by protonation, and (c) the N-terminal amino acid is protected on the amine by the Boc group;--selectively eliminating the group Boc from the N-terminal amine of the peptide in phase of elongation by hydrolysis with trifluoroacetic acid, said coupling being effected in an aprotic polar solvent and--eliminating, at the end of sequence, all the protector groups by hydrolysis with the aid of a 0.1 to 1M solution of methanesulfonic or trifluoromethanesulfonic acid in trifluoroacetic acid.

专利号:US-4797469-A
优先权日:1984-07-10
标 题:Synthesis of hGRF (Somatocrinin) in liquid phase and intermediate peptides
发明人：DIAZ JOSEPH; DEMARNE HENRI; RONCUCCI ROMEO; SCHMELCK PAUL-HENRY
权利人:SANOFI SA
摘要:A process for the synthesis, in liquid phase and by fragments, of hGRF 1-44 and hGRF 1-40. This process consists in coupling, one after the other and in the order of the sequence of the GRF, (1) on the one hand, the following fragments: -H-Ala-Arg-Ala-Arg-Leu-NH2 called Fragment A hGRF (40-44) or - alaninamide (40) -H-Gln-Glu-Arg-Gly-OH called Fragment B'1 hGRF (36-39) -H-Glu-Ser-Asn-OH called Fragment B'2 hGRF (33-35) -H-Ser-Arg-Gln-Gln-Gly-OH called Fragment C hGRF (28-32) -H-Leu-Gln-Asp-Ile-Met-OH called Fragment D' hGRF (23-27) -H-Arg-Lys-Leu-OH called Fragment E'1 hGRF (20-22) - to obtain the peptide K1 [(hGRF (20-44)] on the corresponding peptide having the sequence (20-40) and (2) on the other hand, the following fragments: -H-Gln-Leu-Ser-Ala called Fragment F1 hGRF (16-19) -H-Tyr-Arg-Lys-Val-Leu-Gly OH called Fragment G1 hGRF (10-15) -H-Ile-Phe-Thr-Asn-Ser-OH called Fragment H1 hGRF (5-9) - to obtain the peptide J [hGRF (5-19)] and thereafter to couple together the peptides J and K1 in order to form the peptide having the sequence hGRF (5-44) or hGRF (5-40) and finally to couple the resulting peptide with the peptide H-Tyr-Ala-Asp-Ala-OH, called fragment I hGRF (1-4).

专利号:US-2023295077-A1
优先权日:2020-04-10
标题:An improved process for the preparation of semaglutide side chain
发明人：PANDEY MANEESH KUMAR; SHUKLA SONU PRASAD; NAIN SACHIN; SANDEEP SANDEEP; MALE SRIDHAR; SOKHI SARBJOT SINGH; SINGH GOVIND; LAHIRI SASWATA; CABRI WALTER
权利人:FRESENIUS KABI ONCOLOGY LTD
摘要:The present invention relates to an improved process for the preparation of a compound of Formula (1), The invention also provides improved processes for the preparation of intermediates used in the synthesis of Formula (1). The compound of Formula (1) is used in the synthesis of Semaglutide.

专利号:US-5093530-A
优先权日:1987-03-30
标 题:2,4-dimethoxy-4'-hydroxy-benzophenone
发明人：RINK HANS
权利人:CIBA GEIGY CORP
摘要:A synthetic resin based on a polystyrene that can be used as a support for solid phase peptide synthesis and that has been cross-linked with from 0 to 5 mol % of divinyl benzene, characterized in that it has been substituted at benzene rings of its skeletal structure by groups of the formula ##STR1## in which X represents --O-- or --NH-- and R represents C 1 -C 4 -alkyl, as a support renders possible the solid phase synthesis of peptides and peptide amides that are, if desired, protected at the N-terminal and/or at other functional groups. The resin is manufactured by reaction of a customary chloromethylated polystyrene resin with an alkali metal salt of the corresponding 4-hydroxybenzophenone and subsequent reduction of the carbonyl group and, optionally, amination.

专利号:US-7807140-B2
优先权日:2006-05-03
标题 :Magnetic resonance imaging contrast agents synthesized using ring-opening metathesis polymerization
发明人：KIESSLING LAURA L; RAINES RONALD T; ALLEN MATTHEW J
权利人:WISCONSIN ALUMNI RES FOUND
摘要:Polymeric chelating agents and metal chelates, particularly those of lanthanide metals and more specifically those of Gd(III), useful as contrast agents in magnetic resonance imaging (MRI) for therapeutic and diagnostic applications as well as clinical and biomedical research applications. The polymeric chelates are generated using ring-opening metathesis polymerization (ROMP). Polymers can have multiple sites for functionalization allowing for the synthesis of multimodal and targeted contrast agents. Hydroxypyridonate (HOPO)-based chelating moieties are integrated into a ROMP-derived polymer. More specifically, the HOPO-based chelating moiety is integrated into a benzonorbornadiene unit that constitutes the backbone of the polymer. The ROMP-derived polymer chelators can comprise multiple metal ions, particularly Gd(III) ions, in polymers of varying lengths to provide a series of agents with controlled relaxivites. Polymer chelates include those that are water-soluble.