发明公开
EP0331988A1 Sulfonium compounds, as well as process for producing active esters and amides used for the production of amides
失效
锍化合物和用于制备它们用于制备酰胺的活性酯和酰胺的方法。
- 专利标题： Sulfonium compounds, as well as process for producing active esters and amides used for the production of amides
- 专利标题（中）： 锍化合物和用于制备它们用于制备酰胺的活性酯和酰胺的方法。
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申请号： EP89103237.7申请日： 1989-02-24
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公开(公告)号： EP0331988A1公开(公告)日： 1989-09-13
- 发明人: Kouge, Katsushige
- 申请人： SANSHIN KAGAKU KOGYO CO., LTD.
- 申请人地址： 150, Oaza Yanai Yanai-shi Yamaguchi-ken JP
- 专利权人： SANSHIN KAGAKU KOGYO CO., LTD.
- 当前专利权人： SANSHIN KAGAKU KOGYO CO., LTD.
- 当前专利权人地址： 150, Oaza Yanai Yanai-shi Yamaguchi-ken JP
- 代理机构： Denmark, James
- 优先权： JP55856/88 19880308
- 主分类号： C07C149/46
- IPC分类号： C07C149/46 ; C07C102/06 ; C07K1/08
摘要：
In the present invention an amide represented by the general formula:
is produced using a sulfonium salt represented by the general formula:
as the starting material, to synthesizing a novel compound, i.e., an active ester represented by the general formula:
and further reacting the active ester with a nucleophilic agent represented by the general formula: H-B-Y wherein R 1 represents a hydrogen, an alkyl group or a halogen group; R 2 and R 3 , which may be same or different, each represents an alkyl group; X- represents an anion typified by a halogen ion, a perchloric acid ion, a hydrogen sulfuric acid ion, a methylsulfuric acid ion, and a p-toluenesulfonic acid ion; W represents an alkyl group, alkoxy group
group, in which R 4 . represents a halogen, a hydrogen or a methoxy or a Ci - C 5 alkyl group substituted with 1 - 3 halogen atoms, an aryl group or a fluorenylmethoxy group, or represents, together with W- C -, an amino acid, a peptide, or a protein group, in which the terminal amino group and the side chain group of the amino acid has or has not a protective group, B represents a substituted or not-substituted imino group, Y represents an organic group or B and Y join together to represent a heterocyclic amine. Alternatively H-BY represents an amino acid in which a proper protective group is or is not introduced into a-carboxyl group and/or side chain, or a peptide or protein in which a proper protective group is or is not introduced into the terminal carboxyl group and/or side chain.
is produced using a sulfonium salt represented by the general formula:
as the starting material, to synthesizing a novel compound, i.e., an active ester represented by the general formula:
and further reacting the active ester with a nucleophilic agent represented by the general formula: H-B-Y wherein R 1 represents a hydrogen, an alkyl group or a halogen group; R 2 and R 3 , which may be same or different, each represents an alkyl group; X- represents an anion typified by a halogen ion, a perchloric acid ion, a hydrogen sulfuric acid ion, a methylsulfuric acid ion, and a p-toluenesulfonic acid ion; W represents an alkyl group, alkoxy group
group, in which R 4 . represents a halogen, a hydrogen or a methoxy or a Ci - C 5 alkyl group substituted with 1 - 3 halogen atoms, an aryl group or a fluorenylmethoxy group, or represents, together with W- C -, an amino acid, a peptide, or a protein group, in which the terminal amino group and the side chain group of the amino acid has or has not a protective group, B represents a substituted or not-substituted imino group, Y represents an organic group or B and Y join together to represent a heterocyclic amine. Alternatively H-BY represents an amino acid in which a proper protective group is or is not introduced into a-carboxyl group and/or side chain, or a peptide or protein in which a proper protective group is or is not introduced into the terminal carboxyl group and/or side chain.
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