发明授权
US07026477B1 Process for preparing substituted phenylsulfonylureas from sulfonyl halides 有权
从磺酰卤制备取代苯基磺酰脲的方法

Process for preparing substituted phenylsulfonylureas from sulfonyl halides
摘要:
The invention relates to a preparation process for a compound (I) or a salt thereof, in which Q, X*, Y, Z, R, R1, R2 and R3 are as defined in claim 1, which comprises a) ammonolyzing a comp. (II) in which Hal=halogen atom to give (III), pref. (a1) carrying out the reaction in an organic solvent mixture (org. solv. mixture) comprising (1) opt. halogenated aromatic hydrocarbons and (2) polar aprotic solvents, in a weight ratio of solv. (1): solv. (2) of 20:1 to 1:1, (b) phosgenating the comp. (III) with phenylsulfonyl isocyanate of the formula (IV), pref. (b1) in the case X*=halogen, carrying out the reaction with phosgene in an org. solv. in the presence of isocyanates R′-NCO as catalyst, where R′=(subst.) hydrocarbon, with or without addition of an amine base, (c) reacting the resulting compound (IV) in org. solv. with the aminoheterocycle H2N-Het (Het=heterocycle as in (I)) to give the comp. (I) or a salt thereof, pref. (c1) carrying out the reaction in a solv. mixture of opt. halogenated arom. hydrocarbon having a b.p. of more than 110° C. and a polar aprotic solv., where at least one of the preferred partial steps (a1) to (c1) is carried out in the process.
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