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    PROCESS FOR PREPARATION OF CYCLOPENANE DERIVATIVES
    1.
    发明授权
    PROCESS FOR PREPARATION OF CYCLOPENANE DERIVATIVES 失效

    公开(公告)号：KR790001361B1

    公开(公告)日：1979-09-28

    申请号：KR740002787

    申请日：1974-06-15

    Applicant: HOECHST AG

    Inventor： BECK GERHARD ,  MILOS BABEJ ,  LERCH ULRICH ,  BARTMANN WILHELM

    Abstract: Title compds. (I; R1,R2 = O; R3,R4 = C1-5 alkyl ; R5 = tetrahydropyranyl, H ; U = (CH2)0-5, cis- or trans-alkyl = c-alkyl; V = simple bond, O, furan, benzyl ; W = alkyl-C-alkyl; X = (CH2)0-4), similar in structure to natural prostaglandine, having strong antiprostaglandine activity were prepd. by reaction of II and in aprotic solvent. Thus, 3.66g (5RS,3'RS)-2-oxo-5 3'-(2"-tetrahydropyranyloxy) -trans-1'-octenyl -cyclopentane-carboxylic ester in C6H5CH3 were stirred with 1.35g potassium-t-butylate followed by reaction with 4g 7-iodo-heptanophosphoric ethyl ester to give I.

    PROCESS FOR PREPARING THIENYL-PROSTAGLANDINS
    4.
    发明公开
    PROCESS FOR PREPARING THIENYL-PROSTAGLANDINS 失效

    公开(公告)号：KR830000208A

    公开(公告)日：1983-03-30

    申请号：KR760000522

    申请日：1976-03-04

    Applicant: HOECHST AG

    Inventor： BARTMANN WILHELM ,  REUSCHLING DIETER ,  TEUFEL HERMANN ,  BECK GERHARD ,  SEEGAR KARL

    IPC: A61K31/557 ,  C07D333/16 ,  C07C177/00

    Abstract: Title compds. I(R1,R2 = H, OH; R3 = α- or β-thienyl, α- or β-thienylmethyl, benzo[b thiophene, cyclopentano[b thiopene, cyclohexano[b thiopene; X = C1-7 straight-or sidechain alkylene, C2-8 alkoxyalkylene), exhibiting a hypotension activity and a urination activity, were prepd. by the reaction of lactol (II) and 4-carboxy-butyl-triphenylphosphonium bromide in NaH-dissolved dimethylsulfoxide in the presence of inert gas to give formula acid(II), which was acid hydrolyzed to give compds. I or their esters by eliminating tetrahydropyranyl protecting group.

    PROCESS FOR PREPARING TERT-BUTYL (3R,5S)-6-HYDROXY-3,5-O- ISOPROPYLIDENE-3,5-DIHYDROXYHEXANOATE
    9.
    发明专利
    PROCESS FOR PREPARING TERT-BUTYL (3R,5S)-6-HYDROXY-3,5-O- ISOPROPYLIDENE-3,5-DIHYDROXYHEXANOATE 未知

    公开(公告)号：CA2099444C

    公开(公告)日：2005-03-29

    申请号：CA2099444

    申请日：1993-06-30

    Applicant: HOECHST AG

    Inventor： BECK GERHARD ,  JENDRALLA JOACHIM-HEINER ,  KESSELER KURT

    IPC: C07D319/06

    Abstract: Process for preparing tert-butyl (3R,5S)-6-hydroxy-3,5-O- isopropylidene-3,5-dihydroxyhexanoate A novel process is described for preparing tert-butyl (3R,5S)6-hydroxy-3,5-O-isopropylidene-3,5-dihydroxyhexan- oate of the formula I (See formula I) which is a valuable structural element for preparing inhibitors of HMG-CoA reductase. In particular, the present invention relates to a process for preparing the compound of the formula I, wherein ethyl .omega. benzyloxyacetoacetate of the formula II (See formula II) is asymmetrically hydrogenated at substrate/catalyst molar ratio greater than 1000:1, using an in-situ ruthenium (II) chloride -(R)-BINAP catalyst and hydrogen pressure of less than 5 atm H2 to give ethyl 2(S)-hydroxy-3-benzyloxybutyrate of the formula III, the .beta.-hydroxy ester of the formula III is converted by means of a Claisen condensation into the .beta.-keto-.delta.-(S)-hydroxy ester of the formula IV, the resultant ester of the formula IV is converted by diastereoselective reduction into tert-butyl 3(R),5(S)- dihydroxy-6-benzyloxyhexanoate of the formula V, the hydroxyl groups in the dihydroxy ester of the formula V are protected, with the formation of the acetonide of the formula VI, and the benzyl protective group is removed from the acetonide of the formula VI, with the formation of the compound of the formula I.

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