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1. (WO2001004100) PROCESS FOR PREPARING 2-AMINO-4-(4-FLUORPHENYL)-6-ALKYLPYRIMIDINE-5-CARBOXYLATE
Latest bibliographic data on file with the International Bureau   

Pub. No.: WO/2001/004100 International Application No.: PCT/EP2000/006099
Publication Date: 18.01.2001 International Filing Date: 30.06.2000
Chapter 2 Demand Filed: 22.01.2001
IPC:
C07C 229/34 (2006.01) ,C07C 311/05 (2006.01) ,C07D 239/42 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
C
ACYCLIC OR CARBOCYCLIC COMPOUNDS
229
Compounds containing amino and carboxyl groups bound to the same carbon skeleton
02
having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton
34
the carbon skeleton containing six-membered aromatic rings
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
C
ACYCLIC OR CARBOCYCLIC COMPOUNDS
311
Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
01
Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms
02
of an acyclic saturated carbon skeleton
03
having the nitrogen atoms of the sulfonamide groups bound to hydrogen atoms or to acyclic carbon atoms
05
to acyclic carbon atoms of hydrocarbon radicals substituted by nitrogen atoms, not being part of nitro or nitroso groups
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
239
Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
02
not condensed with other rings
24
having three or more double bonds between ring members or between ring members and non-ring members
28
with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
32
One oxygen, sulfur or nitrogen atom
42
One nitrogen atom
Applicants:
VEITH, Ulrich [DE/CH]; CH (UsOnly)
LONZA AG [CH/CH]; Münchensteinerstrasse 38 CH-4052 Basel, CH (AllExceptUS)
Inventors:
VEITH, Ulrich; CH
Common
Representative:
LONZA AG; Münchensteinerstrasse 38 CH-4052 Basel, CH
Priority Data:
00106303.123.03.2000EP
60/185,37128.02.2000US
60/185,46528.02.2000US
99113711.813.07.1999EP
99120417.314.10.1999EP
Title (EN) PROCESS FOR PREPARING 2-AMINO-4-(4-FLUORPHENYL)-6-ALKYLPYRIMIDINE-5-CARBOXYLATE
(FR) PROCEDE DE PREPARATION DE 2-AMINO-4-(4-FLUORPHENYL)-6-ALKYLEPYRIMIDINE-5-CARBOXYLATE
Abstract:
(EN) Process for the preparation of compounds of general formula (I), in which R is hydrogen or a group of formula -SO2R1 R1 is C1-6-alkyl; R2 is hydrogen or C1-6-alkyl; R3 is C1-6-alkyl; R4 is C1-6-alkyl, characterized in that, in a first stage, a compound of formula (II), in which R3 and R4 have the abovementioned meaning, is reacted in the presence of a Lewis acid with 4-fluoro-benzonitrile to give a compound of general formula (III), in which R3 and R4 have the abovementioned meaning and in a second stage the compound of formula (III) obtained is reacted with the compound of formula (IV), in which R and R2 have the abovementioned meaning, to give the final product of formula (I).
(FR) L'invention concerne un procédé de préparation de composés représentés par la formule générale (I), dans laquelle R représente hydrogène ou un groupe représenté par la formule -SO2R1, où R1 représente alkyle C1-6; R2 représente hydrogène ou alkyle C1-6; R3 représente alkyle C1-6; R4 représente alkyle C1-6, caractérisé en ce que, dans une première étape, on fait réagir un composé représenté par la formule (II), dans laquelle R3 et R4 ont le même sens que ci-dessus, en présence d'un acide de Lewis avec du 4-fluorobenzonitrile afin d'obtenir un composé représenté par la formule générale (III) dans laquelle R3 et R4 ont le même sens que ci-dessus et dans une seconde étape, on fait réagir le composé représenté par la formule (III) ainsi obtenu avec le composé représenté par la formule (IV), dans laquelle R et R2 ont le même sens que ci-dessus, afin d'obtenir le produit final représenté par la formule (I).
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Designated States: AE, AG, AL, AM, AT, AU, AZ, BA, BB, BG, BR, BY, BZ, CA, CH, CN, CR, CU, CZ, DE, DK, DM, DZ, EE, ES, FI, GB, GD, GE, GH, GM, HR, HU, ID, IL, IN, IS, JP, KE, KG, KP, KR, KZ, LC, LK, LR, LS, LT, LU, LV, MA, MD, MG, MK, MN, MW, MX, MZ, NO, NZ, PL, PT, RO, RU, SD, SE, SG, SI, SK, SL, TJ, TM, TR, TT, TZ, UA, UG, US, UZ, VN, YU, ZA, ZW
African Regional Intellectual Property Organization (ARIPO) (GH, GM, KE, LS, MW, MZ, SD, SL, SZ, TZ, UG, ZW)
Eurasian Patent Office (AM, AZ, BY, KG, KZ, MD, RU, TJ, TM)
European Patent Office (EPO) (AT, BE, CH, CY, DE, DK, ES, FI, FR, GB, GR, IE, IT, LU, MC, NL, PT, SE)
African Intellectual Property Organization (BF, BJ, CF, CG, CI, CM, GA, GN, GW, ML, MR, NE, SN, TD, TG)
Publication Language: English (EN)
Filing Language: English (EN)