PROCESS FOR THE PREPARATION OF 2,4-11-DEOXYPGE SERIES PROSTAGLANDIN

    公开(公告)号:KR820000509B1

    公开(公告)日:1982-04-10

    申请号:KR780003626

    申请日:1978-11-30

    Applicant: HOECHST AG

    Abstract: Title compds.(I; R1 = H, C1-10 hydrocarbon, ammonium ion; R2 = C1-6 aliphatic hydrocarbon) were prepd. by the hydrolysis of IV(R3 = protecting group; Z = CH2 or -C(CH3)2 group) obtained from the reaction of II and III (R4 = C1-4 alkyl or phenyl). Thus, 111.2 g 3-carbomethoxy-2-propenyl-2-triphenyl-phosphonium bromide and 71.6 g methyl-γ-bromo-crotonate were stirred at 26oC for 1.5 hr to give I.

    PROCESS FOR THE PREPARATION OF CYCLOPENTANE DERIVATIVES

    公开(公告)号:KR790001979B1

    公开(公告)日:1979-12-30

    申请号:KR790002417

    申请日:1979-09-20

    Applicant: HOECHST AG

    Abstract: Prostaglandin analogues and their intermediates (I; R1 and R2 are different, H or hydroxyl group, R3 = C1-5 alkyl, R4 = C1-5 alkyl, R5 = tetrahydropyranyl of H,U = (CH2)m, m = 0-5, R6 and R7 are same or not, H or C1-5 alkyl group, V = C1-5 alkyl, W =C1-5 alkyl, X = (CH2) m, m = 0-5). The compds, had strong antiprostaglandin activity. Thus, compd. II was reacted with hydrated metal complex to give I.

    PROCESS FOR THE MANUFACTURE OF NOVEL PROSTAGLANDIN ANALOGS

    公开(公告)号:KR820001258B1

    公开(公告)日:1982-07-14

    申请号:KR770003102

    申请日:1977-12-30

    Applicant: HOECHST AG

    Abstract: Title compds. I(R1,R2 = O, H, HO; R3 = H, C1-8 alip. or Cycloalip. group, C7-9 aralip., substituted ammonium ion; R4 = C1-10 alip. hydrocarbon, C3-7 cycloalip. hydrocarbon; R5 = H, alkyl, alkenyl, alkynyl; R6 = H, alkyl; A = trans -CH=CH- or -CH2-CH2-), useful hypertensives, were prepd. by reacting compd. II with acylating agent contg. C2-11 carboxylic group. Thus, 9-keto-15α--hydroxy-16,16-dimethyl-18- oxa -prosta-2,13-dienic acid methyl ester was dissolved in anhydrous dimethoxy ethane and added to a mixt. of dimethoxy ethane, pyridine and acetyl chloride to give 9-keto-15α-acetoxy-16,16-dimethyl-18-oxa-prosta-2,13-dienic acid methyl ester.

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