Global Patent Index - EP 1257540 A1

EP 1257540 A1 2002-11-20 - METHOD FOR THE PRODUCTION OF 1-AMINO-3-ARYL-URACILS

Title (en)

METHOD FOR THE PRODUCTION OF 1-AMINO-3-ARYL-URACILS

Title (de)

VERFAHREN ZUR HERSTELLUNG VON 1-AMINO-3-ARYL-URACILEN

Title (fr)

PROCEDE POUR LA PRODUCTION DE 1-AMINO-3-ARYL-URACILES

Publication

EP 1257540 A1 (DE)

Application

EP 01902351 A

Priority

  • DE 10005284 A
  • EP 0100795 W

Abstract (en)

[origin: DE10005284A1] Preparation of 1-amino-3-phenyl-uracils (I) involves reacting 3-phenyl-uracils (II) with 2-aminooxysulfonyl-1,3,5-trimethylbenzene (III), optionally in presence of a reaction auxiliary and/or a diluent, at -50 to +80 [deg] C. Preparation of 1-amino-3-phenyl-uracils of formula (I) involves reacting 3-phenyl-uracils of formula (II) with 2-aminooxysulfonyl-1,3,5-trimethylbenzene (O-mesitylenesulfonyl-hydro xylamine) of formula (III), optionally in presence of a reaction auxiliary and/or a diluent, at -50 to +80 [deg] C: [Image] R1optionally substituted alkyl; R2H, NO2, CN, halo or optionally substituted alkyl; R3H, NO2, CN or halo; R4H, NO2, CN, CONH2, CSNH2, OH or halo; or alkyl, alkoxy or benzoyloxy (all optionally substituted); R5H, OH, SH, NH2, NHOH, NO2, CN, COOH, CONH2, CSNH2, halo, R6, OR6, NHR6, NHOR6, NHSO2R6, N(SO2R6)2, C(Q1)R7, C(Q1)Q2R6, C(Q1)NHR6, Q2C(Q1)R6, Q2C(Q1)Q2R6, NHC(Q1)R6, N(SO2R6)C(Q1)R6, NHC(Q1)Q2R6 or Q2C(Q1)NHR6; Q : O, S, SO or SO2; Q1, Q2O or S; and R6alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl, aryl, arylalkyl, heterocyclyl or heterocyclylalkyl. - ACTIVITY : None given. - MECHANISM OF ACTION : None given.

[origin: DE10005284A1] The invention concerns a novel method for the production of 1-amino-3-aryl-uracil of formula (I), wherein R<1> represents optionally substituted alkyl; R<2> represents hydrogen, nitro, cyano, halogen or optionally substituted alkyl; R<3> represents hydrogen, nitro, cyano or halogen; R<4> represents hydrogen, nitro, cyano, carbamoyl, thiocarbamoyl, hydroxy, halogen or optionally substituted alkyl, alkoxy or benzoyloxy and R<5> represents hydrogen, hydroxy, mercapto, amino, hydroxyamino, nitro, cyano, carboxy, carbamoyl, Thiocarbamoyl, halogen or one of the following groupings: -R<6>, -Q-R<6>, -NH-R<6>, -NH-O-R<6>, -NH-SO2-R6, -N(SO2R<6>)2, -CQ<1>-R<7>, -CQ<1>-Q<2>-R<6>, -CQ<1>-NH-R<6>, -Q<2>-CQ<1>-R<6>, -Q<2>-CQ<1>-Q<2>-R<6>, -NH-CQ<1>-R<6>, -N(SO<2>-R<6>)-(CQ<1>-R<6>), -NH-CQ<1>-Q<2>-R<6>, -Q<2>-CQ<1>-NH-R<6>, wherein Q represents O, S, SO or SO2, Q<1> and Q<2> independently represent O or S and R represents optionally substituted alkyl, alkenyl, alkinyl, cycloalkyl, cycloalkylalkyl, aryl, arylalkyl, heterocyclyl or heterocyclylalkyl.

IPC 1-7 (main, further and additional classification)

C07D 239/54

IPC 8 full level (invention and additional information)

C07D 239/54 (2006.01)

CPC (invention and additional information)

C07D 239/54 (2013.01)

Citation (search report)

See references of WO 0158883A1

Designated contracting state (EPC)

AT BE CH CY DE DK ES FI FR GB GR IE IT LI LU MC NL PT SE TR

EPO simple patent family

DE 10005284 A1 20010809; AU 3020701 A 20010820; EP 1257540 A1 20021120; JP 2003522762 A 20030729; US 2003032807 A1 20030213; WO 0158883 A1 20010816

INPADOC legal status


2006-02-08 [18D] APPLICATION DEEMED TO BE WITHDRAWN

- Effective date: 20050802

2003-03-12 [17Q] FIRST EXAMINATION REPORT

- Effective date: 20030123

2002-11-27 [RAP1] TRANSFER OF RIGHTS OF AN APPLICATION

- Owner name: BAYER CROPSCIENCE AG

2002-11-20 [17P] REQUEST FOR EXAMINATION FILED

- Effective date: 20020909

2002-11-20 [AK] DESIGNATED CONTRACTING STATES:

- Kind Code of Ref Document: A1

- Designated State(s): AT BE CH CY DE DK ES FI FR GB GR IE IT LI LU MC NL PT SE TR

2002-11-20 [AX] REQUEST FOR EXTENSION OF THE EUROPEAN PATENT TO:

- Free text: AL;LT;LV;MK;RO;SI