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    PROCESS FOR PREPARATION OF CYCLOPENANE DERIVATIVES
    2.
    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.

    1-(Imidazole-1-yl)-isoquinolines and process for preparing them
    4.
    发明授权
    1-(Imidazole-1-yl)-isoquinolines and process for preparing them 失效
    1-（咪唑-1-基） - 异喹啉及其制备方法

    公开(公告)号：US3914236A

    公开(公告)日：1975-10-21

    申请号：US45471374

    申请日：1974-03-25

    Applicant: HOECHST AG

    Inventor： LERCH ULRICH ,  GRANZER ERNOLD

    IPC: A61K31/47 ,  A61K31/472 ,  A61P3/06 ,  A61P3/08 ,  A61P9/10 ,  C07D217/22 ,  C07D217/24 ,  C07D227/06 ,  C07D401/04 ,  C07D521/00

    CPC classification number: C07D231/12 ,  C07D217/22 ,  C07D217/24 ,  C07D233/56 ,  C07D249/08

    Abstract: 1-(1-Imidazolyl)-isoquinolines of the general formula I and their physiologically tolerated salts,

    IN WHICH R1, R2 and R3 represent hydrogen, alkyl of 1 to 4 carbon atoms or phenyl, R1, R2 and R3 may be identical or different, R4 represents hydrogen, alkyl of 1 to 4 carbon atoms, phenyl or chlorine, and R5 represents hydrogen, alkyl of 1 to 6 carbon atoms, cycloalkyl of 5 to 8 carbon atoms, phenyl or chlorine, a process for preparing them and pharmaceutical preparations containing them as active ingredient.

    Abstract translation: 通式I的1-（1-咪唑基） - 异喹啉及其生理上耐受的盐，其中R 1，R 2和R 3表示氢，1至4个碳原子的烷基或苯基，R 1，R 2和R 3可以相同或不同 ，R4表示氢，1-4个碳原子的烷基，苯基或氯，R5表示氢，1-6个碳原子的烷基，5-8个碳原子的环烷基，苯基或氯，它们的制备方法和药物制剂 含有它们作为活性成分。

    PROCESS FOR PRODUCING RACEM AND OPTICALLY ACTIVE 1,2,3,4-TETRAHYDRO-ISOQUINOLINE-3-CARBOXYLIC ACID
    6.
    发明专利
    PROCESS FOR PRODUCING RACEM AND OPTICALLY ACTIVE 1,2,3,4-TETRAHYDRO-ISOQUINOLINE-3-CARBOXYLIC ACID 未知

    公开(公告)号：HU213273B

    公开(公告)日：1997-04-28

    申请号：HU9200231

    申请日：1992-01-24

    Applicant: HOECHST AG

    Inventor： KAMMERMEIER BERNHARD ,  LERCH ULRICH

    IPC: C07D217/26

    Abstract: A process for the preparation of racemic and optically active 1,2.3,4-tetrahydroisoquinoline-3-carboxylic acid is described, in which dihalo-o-xylylenes are cyclized to dicarboxylic acid esters in basic medium using dialkyl N-acylamidomalonates of the formula (CO2R1)2CHNHCOR2, in which R1 is (C1-C4)-alkyl and R2 is H, (C1-C4)-alkyl or (C6-C12)-aryl, decarboxylated by basic hydrolysis and subsequent acid work-up and then reacted in acid medium to give (D,L)-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid, or dihalo-o-xylylenes are cyclized in basic medium to give the dicarboxylic acid esters and these are reacted directly without isolation in a one-pot process to give (D,L)-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid, if desired the racemic 1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid is reacted with (-)menthol and p-toluenesulfonic acid to give (-)menthyl (D)- or (L)-1,2,3,4-tetrahydroisoquinoline-3-carboxylate, then the diastereomers are separated by column chromatography and subjected to basic hydrolysis to give (D)-or (L)-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid, or (D,L)-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid is esterified by means of benzyl alcohol and p-toluenesulfonic acid, reacted with D(-)mandelic acid to give benzyl (D)-1,2,3,4-tetrahydroisoquinoline-3-carboxylate (D)-mandelate and benzyl (L)-1,2,3,4-tetrahydroisoquinoline-3-carboxylate (D)-mandelate or with L(+)mandelic acid to give benzyl (D)-1,2,3,4-tetrahydroisoquinoline-3-carboxylate (L)-mandelate and benzyl (L)-1,2,3,4-tetrahydroisoquinoline-3-carboxylate (L)-mandelate and then the compounds obtained are separated into the optical antipodes by fractional crystallization in an inert solvent and the enantiomers (D)- or (L)-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid are liberated by basic hydrolysis, the chiral auxiliary reagent being recovered.

    10.
    发明专利
    未知

    公开(公告)号：DK162092B

    公开(公告)日：1991-09-16

    申请号：DK343486

    申请日：1986-07-18

    Applicant: HOECHST AG

    Inventor： HENNING RAINER ,  LERCH ULRICH ,  KAISER JOACHIM

    IPC: A61K31/47 ,  A61K31/495 ,  A61K31/535 ,  A61P3/00 ,  A61P3/14 ,  A61P9/00 ,  C07D215/22 ,  C07D215/227 ,  C07D401/12 ,  C07D491/056

    Abstract: Compounds of the formula I (I) where R(1), R(2), R(3), R(4) and R(5) are, inter alia, hydrogen and alkyl, m is 1-4, n is 0 or 1, p is 0-4 and R(6) is identical or different dialkylamine derivatives, and salts thereof, have a calcium-antagonistic action. They are obtained by reacting corresponding amines with a compound II which carries, on the side chain, a leaving group which can be displaced nucleophilically, or from a hydroxyphenyl-dihydroquinolin-2-one compound by reaction with a corresponding side chain compound which has a leaving group which can be displaced nucleophilically.

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