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    4.
    发明专利
    失效

    公开(公告)号：JPS6136827B2

    公开(公告)日：1986-08-20

    申请号：JP18314681

    申请日：1981-11-17

    Applicant: SAGAMI CHEM RES

    Inventor： OSHIMA IWAO ,  HIRAI KENJI

    IPC: C07C231/00 ,  B01J31/00 ,  B01J31/12 ,  B01J31/16 ,  B01J31/20 ,  C07C51/12 ,  C07C67/00 ,  C07C231/12 ,  C07C233/47

    Abstract: A process for the production of an N-acyl- alpha -amino acid represented by the general formula (I) wherein R1, R2, R3 and R4, independently from each other, represent a hydrogen atom, an alkyl or cycloalkyl group which may be substituted, or an aryl or heteroaromatic group selected from the group consisting of furyl, pyrrolyl, pyridinyl, thienyl and indolyl which may be substituted, which comprises reacting an oxirane represented by the general formula (II) wherein R1 and R2 are as defined above, an amide compound represented by the general formula R3CONHR4 (III) wherein R3 and R4 are as defined above, and carbon monoxide in the presence of hydrogen, a cobalt-containing catalyst, and a promoter composed of a compound containing a metal selected from Groups I, II, III and IV of the periodic table.

    DEHYDROTRIPEPTIDE
    9.
    发明专利
    DEHYDROTRIPEPTIDE 失效

    公开(公告)号：JPS58154540A

    公开(公告)日：1983-09-14

    申请号：JP3593182

    申请日：1982-03-09

    Applicant: SAGAMI CHEM RES

    Inventor： OSHIMA IWAO ,  YODA NORIKO

    IPC: C07K5/08 ,  A61K38/00 ,  A61P25/04

    Abstract: NEW MATERIAL:The compound of formulaI(R -R are H, alkyl or aromatic group; Ar is aromatic group). EXAMPLE:N-t-Butoxycarbonylglycyldehydrophenylalanyl-(S)-leucine methyl ester. USE:Block for the synthesis of encephaline analogue. PROCESS:The objective peptide can be prepared by reacting the dipeptide of formula II (e.g. N-t-butoxycarbonylglycyl-DL-phenylserine) with sodium acetate in the presence of acetic anhydride, and reacting the resultant compound of formula III (e.g. 2-butoxycarbonylaminomethyl-4-benzylidene-5-oxazolone) with the alpha-aminoacid of formula IV or its ester e.g. (S)-leucine methyl ester hydrochlororide .

    PREPARATION OF N-ACYL-ALPHA-AMINOACID
    10.
    发明专利
    PREPARATION OF N-ACYL-ALPHA-AMINOACID 失效

    公开(公告)号：JPS5869853A

    公开(公告)日：1983-04-26

    申请号：JP16637681

    申请日：1981-10-20

    Applicant: SAGAMI CHEM RES

    Inventor： OSHIMA IWAO ,  HIRAI KENJI

    IPC: C07B61/00 ,  B01J23/00 ,  B01J23/74 ,  B01J23/89 ,  C07C67/00 ,  C07C231/00 ,  C07C231/08 ,  C07C231/10 ,  C07C231/18 ,  C07C233/46 ,  C07C233/47 ,  C07C233/49 ,  C07C233/83 ,  C07C233/85

    Abstract: PURPOSE:The reaction between an alcohol derivative, an amide and carbon monoxide is effected in the presence of cobalt and a platinum group metal catalyst, to produce the titled compound from inexpensive and readily available raw materials through the one-stage process in high yield. CONSTITUTION:The reaction between an alcohol derivative of formulaI (R , R , R are H, alkyl, aryl; n is 1, 2), an amide of R CONHR (R means the same as R -R ; R is H, alkyl) and carbon monoxide is conducted in a solvent such as tetrahydrofuran or benzene in the presence of a catalyst consisting of cobalt compound such as Co2(CO)8 and a compound of a platinum group metal such as RhCl3.3H2O, preferably under 1-100 atmospheric pressure of hydrogen at 100-200 deg.C to give the objective compound of formula II (m is 0, 1).

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