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    6.
    发明专利
    未知

    公开(公告)号：DE2835439A1

    公开(公告)日：1980-02-28

    申请号：DE2835439

    申请日：1978-08-12

    Applicant: BASF AG

    Inventor： KOENIG HORST DIPL CHEM DR ,  FRANKE ALBRECHT DIPL CHEM DR ,  FRICKEL FRITZ-FRIEDER DIPL CHE ,  STEGLICH WOLFGANG PROF DIPL CH ,  ENGEL NORBERT DIPL CHEM

    IPC: C07D207/32 ,  C07D207/333

    Abstract: 2-(o-Hydroxyphenyl)-pyrrole and a process for its preparation, wherein o-benzyloxybenzoic acid allylamide is reacted with phosgene in an inert solvent, the resulting imide-chloride is cyclized in the presence of a strong sterically hindered base and the benzyl protective group is then removed by hydrogenolysis. 2-(o-Hydroxyphenyl)-pyrrole is a valuable intermediate for the synthesis of drugs. In particular, alkylamino-hydroxypropyl ethers thereof can, because of their beta -sympatholytic actions, be used for the treatment of coronary cardiac diseases, cardiac arrhythmias and hypertonia.

    Diastereomeric 4,4-di:substd.-2-imidazolin-5-one derivs. - prepd. by asymmetric induction, intermediates for optically pure aminoacid(s) such as methyl-DOPA
    7.
    发明专利
    Diastereomeric 4,4-di:substd.-2-imidazolin-5-one derivs. - prepd. by asymmetric induction, intermediates for optically pure aminoacid(s) such as methyl-DOPA 未知

    公开(公告)号：DE2658942A1

    公开(公告)日：1978-07-06

    申请号：DE2658942

    申请日：1976-12-24

    Applicant: BASF AG

    Inventor： SCHOELLKOPF ULRICH ,  HAUSBERG HANS-HEINRICH DIPL CH ,  MAY HANS-JOACHIM DIPL CHEM DR ,  KOENIG HORST DIPL CHEM DR

    IPC: C07D233/70

    Abstract: Imidazoline-5-one derivs. of formula (I) are new: R1 is the optical active residue of a primary amine or aminoacid. R2 is H, 1-4C alkyl, benzyl or phenyl. R3 is 1-4C alkyl (opt. substd. by alkoxy, alkylthio or dialkyamino (all 1-4C alkyl), benzyloxy, benzylthio, 1-4C acyloxy, CN, 2-5C carbalkoxy, benzoyl or phenyl (the rings opt. substd. by 103 halo, NO2, 1-4C alkyl, alkoxy, or alkylthio, benzyloxy, 1-4C acyloxy or acylamino, or by one phenoxy (itself opt. substd by 1-4C alkoxy or acyloxy), CF3 or methylenedioxy), or R3 is allyl or phenyl. R4 is 1-6C alkyl opt. substd. by alkoxy, alkylthio or dialkylamino (all 1-4C alkyl), piperidino, pyrrolidino, benzyloxy, benzylthio, CN, 2-5C carbalkoxy, benzoyl or phenyl (both opt. substd. as for corresp. gps. R3), or R4 is ClCH2 or allyl. Q is pyridyl, furyl, thienyl, naphthyl, benzothienyl or bromobenzofuran. Where R3 and R4 are different, (I) are intermediates (by conventional hydrolysis) for optically active alpha-e ethyl-arylalanines, e.g. alpha-methyl-dopa (an antihypertensive) and alpha-methyltyrosine (a tranquilliser). (I) are prepd. by alkylation of corresp. cpds. (I) where R4 is H alkylation at the 4-posn. proceeds with nearly 100% asymmetric induction (the nature of R1 determines the configuration at this position) and practically no O-alkylation occurs. In an example, 1-L-alpha-phenylethyl-4-methyl-4-benzyl-2-imidazoline-5-one was prepd. from the L-alpha-phenylethylamide of alpha-isocyanopropionic acid/n-BuLi and benzyl bromide.

    9.
    发明专利
    未知

    公开(公告)号：DE2451725A1

    公开(公告)日：1976-05-13

    申请号：DE2451725

    申请日：1974-10-31

    Applicant: BASF AG

    Inventor： KOENIG HORST DIPL CHEM DR ,  BOELL WALTER DIPL CHEM DR

    IPC: C07D263/32

    Abstract: 4-Methyloxazole is manufactured by reaction of formimido-esters with hydroxyacetone. 4-Methyloxazole, manufactured by the process of the invention, is a starting material for the manufacture of dyes, pharmaceuticals, pesticides and vitamins.

    10.
    发明专利
    未知

    公开(公告)号：DE2408288A1

    公开(公告)日：1975-09-04

    申请号：DE2408288

    申请日：1974-02-21

    Applicant: BASF AG

    Inventor： AMANN AUGUST DR MED ,  KOENIG HORST DIPL CHEM DR ,  THIEME PETER C DIPL CHEM DR ,  GIERTZ HUBERT PROF DR MED ,  KRETZSCHMAR ROLF DR

    IPC: C07D285/12 ,  A61K31/41 ,  A61K31/433 ,  A61P25/08 ,  C07D285/125

    Abstract: 1494757 1,3,4-Thiadiazolium compounds BASF AG 20 Feb 1975 [21 Feb 1974] 7106/75 Heading C2C The invention comprises novel compounds (I) in which (a) R 2 , R 3 , R 4 , R 5 and R 6 are identical or different and are hydrogen, fluorine, chlorine, bromine, iodine, alkyl of 1 to 4 carbon atoms, alkoxy of 1 to 4 carbon atoms in the alkyl moiety, trifluoromethyl or NO 2 , at least one of the substituents R 2 to R 6 being different from hydrogen, and R 1 is alkyl or 2 to 6 carbon atoms which is optionally substituted by OH, CN, phenyl or cycloalkyl of 3 to 6 carbon atoms in the ring, or (b) R 1 is methyl optionally substituted by phenyl or cycloalkyl of 3 to 6 carbon atoms in the ring when at least two of R 2 to R 6 are different from hydrogen, or, when R 2 , R 3 , R 5 and R 6 have the above meanings, R 4 is hydrogen, fluorine, bromine, iodine, alkyl of 2 to 4 carbon atoms, alkoxy of 2 to 4 carbon atoms in the alkyl moiety, trifluoromethyl or NO 2 and at least one of R 2 , R 3 , R 4 , R 6 and R 6 is different from H, or (c) R 2 , R 3 , R 4 , R 5 and R 6 are each hydrogen when R 1 is alkyl of 3 to 6 carbon atoms which is optionally substituted by OH, CN, phenyl or cycloalkyl of 3 to 6 carbon atoms in the ring or when R 1 is ethyl which is #-substituted by OH, CN, phenyl or cycloalkyl of 3 to 6 carbon atoms in the ring, or (d) R 1 is methyl substituted by cycloalkyl of 3 to 6 carbon atoms in the ring when R 2 , R 3 , R 4 , R 5 and R 6 are each hydrogen or R 2 , R 3 , R 5 and R 6 are hydrogen and R 4 is chlorine. They are made by reacting compounds (II) (obtained by reacting compounds III with R 1 NHNH 2 ; the free acids corresponding to III are also prepared as are compounds IV) with carbon disulphide or thiophosgene. Pharmaceutical preparations having anticonvulsive action contain (I) as active ingredient. Administration is preferably orally.

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