公开(公告)号：DE3011327A1

公开(公告)日：1981-10-01

申请号：DE3011327

申请日：1980-03-24

Applicant: BASF AG

Inventor： MAY HANS-JOACHIM DIPL CHEM DR ,  LENKE DIETER PROF DR ,  GRIES JOSEF DR ,  TESCHENDORF HANS-JUERGEN DR ,  WORSTMANN WOLFGANG DR

IPC: C07D409/06 ,  A61K31/33 ,  A61K31/415 ,  A61K31/465 ,  A61K31/47 ,  A61P9/08 ,  A61P9/10 ,  A61P9/12 ,  A61P43/00 ,  C07D233/54 ,  C07D233/64 ,  C07D401/06 ,  C07D403/06 ,  C07D405/06 ,  C07D413/06 ,  C07D417/06 ,  C07D233/50 ,  C07D401/12 ,  C07D405/12 ,  C07D407/12 ,  C07D409/12 ,  A61K31/435 ,  A61K31/42 ,  A61K31/425

Abstract: 1-Aroyl-2-phenylamino-2-imidazolines of the general formula where R1 and R2 are identical or different and each is chlorine, bromine, fluorine, methyl, ethyl, methoxy, trifluoromethyl or cyano, R3 has the meanings given for R1 and R2 or is hydrogen and Ar is an unsubstituted or substituted monocyclic or bicyclic heteroaromatic radical containing 1, 2 or 3 nitrogen and/or oxygen and/or sulfur atoms, their salts with physiologically tolerated acids, their preparation, and drugs containing these compounds. The compounds have, inter alia, a blood pressure-reducing action.

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.

公开(公告)号：DE2430354A1

公开(公告)日：1976-01-15

申请号：DE2430354

申请日：1974-06-25

Applicant: BASF AG

Inventor： MAY HANS-JOACHIM DIPL CHEM DR ,  KRETZSCHMAR ROLF DR ,  NEUMANN WOLFGANG DR

IPC: C07D209/44 ,  C07D401/12 ,  C07D405/12 ,  C07D491/056 ,  A61K31/40