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Improved processes for the preparation of compounds 1 - 5 - alkyl aryl pyrazole
专利权人:
MERIAL LIMITED
发明人:
CHARLES Q. MENG,XINXI ZHAN,MICHEL MULHAUSER,JEAN LABROSSE,LOIC ROBERT - LE HIR DE FALLOIS,HYOUNG LEE
申请号:
ARP130101318
公开号:
AR090773A1
申请日:
2013.04.22
申请国别(地区):
AR
年份:
2014
代理人:
摘要:
1. Claim 1: a preparation process for preparing 1-aril-5-alkylpyridinazole (1),Among them: r74955 is hydrogen, cyanogen, halogen, r831222; 74955;formilo -CO H C (O) R-C (O) ORC (O) NR R o -C (S) NHR es R o -S (O) RR³ᵇ is alkyl, haloalkyl, hydroxyalkyl, cycloalkyl, halocycloalkyl, alkenyl, alkynyl, aryl, heterocyclyl, heteroaryl, R⁸ᵇNH, (R⁸ᵇ) ₂N, R⁸ᵇO, R⁸ᵇS or R⁸ᵇC (O) CH₂- where each alkyl, cycloalkyl, alkenyl group, aryl, heterocyclyl or heteroaryl can be optionally substituted with one or more halogen, hydroxy, alkoxy, alkoxyalkoxy, amino, alkylamino, dialkylamino, nitro, cyano or -C (S) NH₂;R⁴ᵇ,R⁵ᵇ,R8311; - 7495y and R3 74955 are independent bodies between hydrogen, halogen, tar, halotar, cyanogen or nitrogen; r8310; - 7495s are halogen, tar, halogenated tar, alcox, Hal alcoxi, cyanogen, nitrogen, - C (o) R1 square 74955;S (O) R o SFW is nitrogen or C-R¹³ᵇ;R⁸ᵇ is alkyl, haloalkyl, hydroxyalkyl, cycloalkyl, halocycloalkyl, alkenyl, haloalkenyl, alkynyl, haloalkynyl, aryl, heterocyclyl, or heteroaryl; R⁹ᵇ and R¹⁰ᵇ are independently hydrogen, alkyl, haloalkyl, hydroxy or alkoxy; R¹¹ᵇ is alkyl, haloalkyl, alkenyl, haloalkenyl, haloalkynyl, cycloalkyl, or halocycloalkyl; R¹²ᵇ is alkyl or haloalkyl; m is 0, 1 or 2; and n is 0, 1 or 2; comprising: (i) reacting a compound of formula (2),At R74955,74955,R⁴ᵇ,R⁵ᵇ,R⁶ᵇ,R8311;; 74959 and W are the iodine, bromine, chlorine or halosulfinyl sulfonyl arylates of compounds (1) and Q of the above formula; the compounds are R-M or formula (3),where R, R¹ᵈ,R y R son en forma independiente alquilo haloalquilo cicloalquilo halocicloalquilo alquenilo alquinilo arilo heteroarilo o heterociclilo donde cada grupo alquilo cicloalquilo alquenilo alquinilo arilo heteroarilo o heterociclilo puede estar opcionalmente sustituido con uno oms grupos hal geno hidroxi alcoxi alcoxialcoxi amino alquilamino dialquilamino nitro ciano o -C ( M is MGX, ZnX, rzn, by832222,Bf8323 or snr83223;X is iodine, bromine or chlorine; it is Oh or alcoxi, or each of
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