PRODUCTION OF PEPTIDE
    5.
    发明专利

    公开(公告)号:JPH0249799A

    公开(公告)日:1990-02-20

    申请号:JP8653889

    申请日:1989-04-05

    IPC分类号: C07D233/64 C07K1/06 C07K14/00

    摘要: PURPOSE:To obtain peptides using a protecting group capable of removal under so mild conditions as to be stable against acids, bases and reduction by protecting a imidazole group of histidine with 4-methoxy-2,3,6-trimethylbenzenesulfonyl group and synthesizing a peptide. CONSTITUTION:In production of a peptide containing histidines, imidazole groups of the histidines are reacted with 4-methoxy-2,3,6-trimethylbenzenesulfonyl chloride to form histidine derivatives represented by the formula (R is H or protective group of-amino group; 4-Methoxy-2,3,6-trimethylbenzenesulfonyl group is bonded to N at 1 or 3 position of A ring.) where each imidazole group is protected with a 4-methoxy-2,3,6-trimethylbenzenesulfonyl group and then peptide condensation is carried out. The protecting groups are subsequently removed using an acid or 1-hydroxybenzotriazole to produce the objective peptide.

    ARGININE DERIVATIVE
    7.
    发明专利

    公开(公告)号:JPS63211262A

    公开(公告)日:1988-09-02

    申请号:JP2824488

    申请日:1988-02-09

    摘要: NEW MATERIAL:A compound shown by formula I (R1 and R5 are CH3 or OCH3; R2 and R4 are CH3 or H; R3 is CH3 or OCH3; R6 is H or alpha-amino protecting group) and a salt thereof. USE:An intermediate for producing peptide. PREPARATION:alpha-Amino group of arginine is protected with carbobenzoxy group, etc., and the resultant substance is reacted with a halogenide containing a substituted benzenesulfonyl group shown by formula II at -5-10 deg.C to give a compound shown by formula I. The reaction is preferably carried out in the presence of a base such as NaOH, etc., in a solvent such as water, acetone, DMF or THF.

    S-FARANESYLPEPTIDE
    9.
    发明专利

    公开(公告)号:JPS625995A

    公开(公告)日:1987-01-12

    申请号:JP14463386

    申请日:1986-06-19

    摘要: NEW MATERIAL:The compound of formula H-Tyr-Pro-Glu-Ile-Ser-Trp-Thr-Arg- Asn-Gly-Cys(S-farnesyl)-N-H2 wherein the C-terminal may be carboxylic acid. USE:It has the activity to promote the formation of conjugating tube and is useful for the breeding of yeast and improvement of species and as a biochemical reagent, etc. PREPARATION:For example 1, equivalent of the peptide of formula H-Tyr-Pro- Glu-Ile-Ser-Trp-Thr-Arg-Asn-Gly-Cys-OH (or -NH2) is made to react with prefer ably 2-4 equivalent of farnesyl bromide in a hydrous DMF solvent (preferably having a water-content of 30-60 vol%) in the presence of preferably 2-4 equiva lent of magnesium oxide at 0-30 deg.C for 3-12hr.