公开(公告)号：DE3211851A1

公开(公告)日：1983-10-06

申请号：DE3211851

申请日：1982-03-31

Applicant: BASF AG

Inventor： ACKER ROLF-DIETER DIPL CHEM DR ,  ROSSY PHILLIP A DIPL CHEM DR ,  HAMPRECHT GERHARD DIPL CHEM DR ,  WUERZER BRUNO

IPC: A01N47/36 ,  C07D333/38

Abstract: Dihydrothiophenecarboxylates of the formula where R1 and R2 have the meanings given in the description, are used for controlling undesirable plant growth.

公开(公告)号：DE3124699A1

公开(公告)日：1983-01-13

申请号：DE3124699

申请日：1981-06-24

Applicant: BASF AG

Inventor： ROSSY PHILLIP A DIPL CHEM DR ,  THYES MARCO DIPL CHEM DR ,  FRANKE ALBRECHT DIPL CHEM DR ,  KOENIG HORST PROF DIPL CHEM DR ,  GRIES JOSEF DR MED ,  LEHMANN HANS DIETER DR MED ,  LENKE DIETER PROF DR

IPC: A61K31/50 ,  A61K31/55 ,  A61P7/02 ,  A61P9/12 ,  C07D209/34 ,  C07D215/22 ,  C07D215/227 ,  C07D223/16 ,  C07D401/04 ,  C07D403/04 ,  C07D403/10 ,  A61K31/40 ,  A61K31/47 ,  C07D401/10

Abstract: 2-Aryl-3,4-diazabicyclo[4.n.O]alk-2-en-5-ones of the formula I I where m and n are identical or different and each is 1, 2 or 3, and R, R1 and R2 are identical or different and each is hydrogen or alkyl of 1 to 6 C atoms, said compounds are useful for treating high blood pressure and thrombo-embolic disorders.

公开(公告)号：DE3209159A1

公开(公告)日：1983-09-15

申请号：DE3209159

申请日：1982-03-13

Applicant: BASF AG

Inventor： ROSSY PHILLIP A DIPL CHEM DR ,  THYES MARCO DIPL CHEM DR ,  FRANKE ALBRECHT DIPL CHEM DR ,  KOENIG HORST PROF DIPL CHEM DR ,  GRIES JOSEF DR MED ,  LEHMANN HANS DIETER DR MED ,  LENKE DIETER PROF DR

IPC: A61K31/50 ,  A61K31/502 ,  A61P7/02 ,  A61P9/12 ,  C07D237/04 ,  C07D237/26 ,  C07D237/14

Abstract: 6-Aryl-4,5-dihydro-3(2H)-pyridazinones of the formula (I) where R is hydrogen, R1 is hydrogen or C1-C3-alkyl, or R and R1 together are methylene, R2 and R3 are identical or different and are each hydrogen or C1-C6-alkyl, and A is hydroxyl, C1-C6-alkoxy, C2-C7-acyloxy, a C2-C7-carbamic acid ester group, C1-C6-alkylsulfonyloxy, C1-C6-alkylmercapto, carboxyl, C2-C7-alkoxycarbonyl or nitrile, and their preparation are described. The substances are suitable for treating disorders.

公开(公告)号：DE3018109A1

公开(公告)日：1981-11-19

申请号：DE3018109

申请日：1980-05-12

Applicant: BASF AG

Inventor： ROSSY PHILLIP A DIPL CHEM DR ,  VOGEL FRIEDRICH DIPL CHEM DR

IPC: C07D333/36 ,  C07D495/04 ,  C07D495/06

Abstract: In the prodn. of biotin, (A) a 2-formyl-3,4- diaminothiophene (I) is subjected to Wittig reaction with a carboxypropylidene-phosphorane (II); (B) the resulting 5-(3,4-diaminothienyl)-pentenoic or -pentadienoic acid deriv. (III) is hydrogenated in a conventional manner; (C) the protecting groups R1-R4 are removed from the resulting tetrahydrothiophene deriv. (IV) by saponification or hydrogenolysis. and (D) if necessary the intermediately formed diamine deriv. is converted into biotin by reaction with phosgene. In the formulae R1-R4 are H or a usual amino-protecting group removable by acidic or basic hydrolysis or hydrogenolysis; or R1 and R3 together represent a carbonyl group; and R5 is lower alkyl, triarylsilyl or acyl. Biotin (vitamin H) is essential for human nutrition. The hydrogenation steps give an all-cis product, so that racemic biotin is obtd. free from other diastereomers.

公开(公告)号：DE3209158A1

公开(公告)日：1983-09-15

申请号：DE3209158

申请日：1982-03-13

Applicant: BASF AG

Inventor： ROSSY PHILLIP A DIPL CHEM DR ,  THYES MARCO DIPL CHEM DR ,  FRANKE ALBRECHT DIPL CHEM DR ,  KOENIG HORST PROF DIPL CHEM DR ,  GRIES JOSEF DR MED ,  LEHMANN HANS DIETER DR MED ,  LENKE DIETER PROF DR

IPC: C07D237/04 ,  C07D237/14 ,  A61K31/50

Abstract: Compounds of the general formula in which R denotes a hydrogen atom or the methyl, ethyl or propyl radical and R , if R denotes a hydrogen atom, denotes an alkenyl radical having 3 to 8 C atoms, which is optionally substituted by 1 to 3 halogen atoms, excluding the 1-methylvinyl radical, or, if R denotes the methyl, ethyl or propyl group, denotes an alkenyl radical having 2 to 8 C atoms, which is optionally substituted by 1 to 3 halogen atoms, and therapeutic compositions which contain these compounds.

公开(公告)号：DE3135617A1

公开(公告)日：1983-03-17

申请号：DE3135617

申请日：1981-09-09

Applicant: BASF AG

Inventor： ROSSY PHILLIP A DIPL CHEM DR ,  THYES MARCO DIPL CHEM DR ,  FRANKE ALBRECHT DIPL CHEM DR ,  KOENIG HORST PROF DIPL CHEM DR ,  GRIES JOSEF DR MED ,  LEHMANN HANS-DIETER DR MED ,  LENKE DIETER PROF DR

IPC: C07D237/26 ,  A61K31/50

Abstract: The present invention relates to diazabicyclo[4.2.0]octenones of the formula I, in which Y has the meaning given in the description, to their preparation and to their use as medicaments in the treatment of high blood pressure and for the therapy of thromboembolic disorders.

公开(公告)号：DE3018134A1

公开(公告)日：1981-11-19

申请号：DE3018134

申请日：1980-05-12

Applicant: BASF AG

Inventor： ROSSY PHILLIP A DIPL CHEM DR ,  VOGEL FRIEDRICH DIPL CHEM DR

IPC: C07D333/38 ,  C07D333/42 ,  C07D495/04 ,  C07F7/10 ,  C07D495/06 ,  C07F7/18

Abstract: New 3,4-diamino-thiophene-2-carboxylic acid esters are of formula (I): (where R1-R4 are H or usual amino- protecting gps. removable by acidic or basic hydrolysis or by hydrogenolysis; or R1 and R3 together represent a carbonyl gp.; and R5 is lower alkyl, benzyl, trialkylsilyl or tert-butyl). (I) are useful as intermediates for biotin, pharmaceuticals and dyes. Conversion into biotin is effected by redn. and partial oxidn. to 3,4-diamine-1- formyl- thiophene cpds., Wittig reaction with a phosphorane deriv. to introduce the biotin side-chain, hydrogenation of the prod. and cyclisation with phosgene. Specifically claimed is 3,4-diamino-2- carbomethoxy- thiophene; 3,4-di(2-oxo-imidazolido)-2- carbomethoxy- thiophene; and 3 other cpds.

公开(公告)号：DE2714896A1

公开(公告)日：1978-10-12

申请号：DE2714896

申请日：1977-04-02

Applicant: BASF AG

Inventor： ROSSY PHILLIP A DIPL CHEM DR ,  BAUMANN MANFRED DIPL CHEM DR ,  HOFFMANN WERNER DIPL CHEM DR

IPC: C07D307/58 ,  C07D307/32

Abstract: New 3-oxo-4-dimethylaminomethylidene-tetrahydrofurans have formula (I): (where R1 and R2 are H, Me or Et). The use of (I) to prepare 3,4-dioxo-tetrahydrofurans having formula (IV), by oxidn. with singlet-O, is claimed. (I) can be used as aromatising materials and have a malty, bread-like odour, similar to, but weaker than, that of (IV). (IV) are known aroma materials. (I) can be prepd. economically, in good yields, e.g. 80-90%. Conversion to (IV) is quantitative. In an example, 3-oxo-2,5-dimethyl-4-dimethylamino-methylidene tetrahydrofuran was prepd. by stirring 3-oxo-2,5-dimethyl-tetrahydrofuran with either (a) tert. butoxy-bis-(dimethylamino)-methane or (b) N,N-dimethyl-formamide-dimethyl acetal.

公开(公告)号：DE2700262A1

公开(公告)日：1978-07-13

申请号：DE2700262

申请日：1977-01-05

Applicant: BASF AG

Inventor： ROSSY PHILLIP A DIPL CHEM DR ,  HOFFMANN WERNER DIPL CHEM DR

IPC: C07D333/32 ,  C07D333/36 ,  C07D333/38 ,  C07D495/04

Abstract: Prepn. of thiophenes of formula involves (i) dehydrogenation of dihydrothiophenes of formula (II) by means of phosphoric acid chloride or bromide SO2Cl2, SO2Br2, Cl2, Br2, I2, or R10 -CO-N(X)-R9 or (ii) dehydrogenation of disulphido-(3,3')-bis-(dihydrothiophenes) of formula (III): or of dihydrothiophenes of formula (IV) by means of SO2Cl, SO2Br2 or Cl2. In the formula R1 is a gap. (V):- R3-O-, R3-S-, r3-2N-, R3-SO3-, R3-CO-S- or R3-CO-O-; R2 is -CO-OR3, -CN, -CO-NR32 or -CO-R4; R3 and R4 are (cyclo)aliphatic, araliphatic or aromatic gps, and R3 may also be H; R1 and R2 may also together form a gp. R5 is H; R6 is -N-R8, -O-, or -S-; R7 is a (cyclo)aliphatic araliphatic or aromatic gp., or R5 and R7 may form, with the 2 adjacent C atoms, part of an aromatic residue; R8 is H or an aliphatic gp.; R9 is H or -CO-R10-R10 is an (ar)aliphatic or aromatic gp., or 2 R10 gps. may form together a -CO-R11 or -NX-C(R3)2-CO- gp.; R11 is an alkylene gp.; R12 has the same meaning as R1; R13 has the same meaning as R12 or when R12 is (V), R13 may be a gp.: X is Cl or Br; and n = 0 or 1.

公开(公告)号：DE2700261A1

公开(公告)日：1978-07-13

申请号：DE2700261

申请日：1977-01-05

Applicant: BASF AG

Inventor： ROSSY PHILLIP A DIPL CHEM DR ,  HOFFMANN WERNER DIPL CHEM DR ,  MUELLER NORBERT DIPL CHEM DR

IPC: C07D333/38

Abstract: Prepn. of thiophen carboxylic acids of formula (I) is effected by reaction of a 3-ketothiphan carboxylic acid (II) with a sulphonic acid: R4. SO2Y (III) to give a 3-sulphato deriv. then reacting the product with an alkali metal polysulphide. The resulting cpd. is treated with a sulphuric acid chloride or bromide or with Cl2 to give modified polysulphide which is finally treated with ahalogen and water. In the formula R is CO2R3 or H; R2 is H whe R' is -CO2R3; or R' is -CO2R3 when R' is H; R3 is H or an aliphatic group; X is halo; R4 is an aliphatic or aromatic group; Y is halo, the group OR3 or a group -O3S.R4. Provides simple, more economic process for prodn. of (I) which is intermediate for thiophen-saccharin sweetening agents. A typical cpd. methyl-3-chlorosulphonylthiophen-4-carboxylate, was prepd. by the 4-stage process from methyl 3-hydroxy-dihydrothiophen-4-carboxylate.