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.

    PROCESS FOR PREPARING ISOQUINOLINE DERIVATIVES

    公开(公告)号:KR820002385B1

    公开(公告)日:1982-12-29

    申请号:KR790001318

    申请日:1979-04-25

    Applicant: HOECHST AG

    Abstract: Isoquinolines I(R1 = amino group -N(R4)(R5); R4, R5 = alky1 and make 5-8 membered cycle with N; R2 = halogen, OH, nitro, amino, substituted amino, mono- or di-substituted pheny1, pyridy1 or thieny1; R3 = H, OH, halogen, C1-6 alky1, alkoxy, NO2, amino, ethylenedioxy; m = 1,2), exhibiting effective activities for melancholia, were prepd. by reacting compds. II (X = H, carboxy1; Y = cl, Br) with amines (III). Thus, 3-chloro-1-pheny1-isoquinoline-4-carboxylic acid was heated to 150oC in N-methy1-piperazine and maintained for 6 hr to give 3-N-methy1piperazino-1-pheny1-isoquinoline.

    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.

    BASICALLY SUBSTITUTED INDOLE DERIVATIVES

    公开(公告)号:KR800001398B1

    公开(公告)日:1980-12-02

    申请号:KR760003232

    申请日:1976-12-30

    Applicant: HOECHST AG

    Abstract: The indole derivs. (I; R1 = pyrrolidino, piperidino, 4-hexamethyleneimino, morphorino, 4-hydroxypiperidino, 4-carbethoxy-piperidino, 1-piperaziny1; R2 = H, pyrrolidino, hexamethylene-imino, 4-hydroxypiperidino, morpholino, 1-piperazinyl; R3 = H, 6-methoxy; m= 1-2; R4 = H, Me, Ph, benzyl, alkoxypheny1), useful as hypotensive and antiarrhythmics, were prepd. by reaction of II(R = Cl, Br) and HNR5R6(R5, R6 = C1-6 alkyl). Thus, 51.2g II(R = Cl) was refluxed with 172g anhydrous piperazine in 500ml dioxane to give 46g 1-pheny1-2-piperazino-3-indole carbaldehyde.

    PROCESS FOR THE PREPARATION OF PROST ANOIC ACID

    公开(公告)号:KR790001860B1

    公开(公告)日:1979-12-26

    申请号:KR740003673

    申请日:1974-09-23

    Applicant: HOECHST AG

    Abstract: Prostanoic acid [I; u= (CH2)m, m = 0-5, - R3CCR4-, (R3 = / ≠ R4 = H, C1-C5 alkyl, but when X is (CH2)1-3, R3,R4 ≠ H at the same time), V= single bond, O, W = R5CR6 (R5 = / ≠ R6 = 0), C1-C5 alkyl) and its acid salts useful as anticonvulsive, were prepd. by retro-Dieckmann condensation of II to give III, followed by alkali safonification of III, decarboxylating, and then isolating ethers from III.

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