摘要:
A process for preparing 4,6-dichloropyrimidine is described, comprising treating 4,6-dihydroxypyrimidine with phosphorus oxychloride in the presence of a saturated hindered amine, the hydrochloride salt of a saturated hindered amine, or an unsaturated 5-membered nitrogen containing ring or a mixture thereof, and, as a first step, directly extracting the 4,6-dichloropyrimidine so formed.
摘要:
4,6-Dichloropyrimidine is prepared by treating 4,6-dihydroxypyrimidine with a chlorinating agent of the formula R.sup.1 R.sup.2 R.sup.3 PCl.sub.2 wherein R.sup.1, R.sup.2 and R.sup.3 are independently alkyl or aryl, or one or more of the groups R.sup.1, R.sup.2 and R.sup.3 is linked to a polymer support. Conveniently, the chlorinating agent may be prepared in situ by reacting the corresponding phosphine oxide with phosgene. Thus, in a preferred process, 4,6-dichloropyrimidine is prepared by treating 4,6-dihydroxypyrimidine with phosgene in the presence of a phosphine oxide.
摘要翻译:通过用式R 1 R 2 R 3 PCl 2的氯化剂处理4,6-二羟基嘧啶来制备4,6-二氯嘧啶,其中R 1,R 2和R 3独立地是烷基或芳基,或者R 1,R 2和R 3中的一个或多个与 聚合物支持。 方便地,氯化剂可以通过使相应的氧化膦与光气反应而原位制备。 因此,在优选的方法中,通过在氧化膦存在下用光气处理4,6-二羟基嘧啶来制备4,6-二氯嘧啶。
摘要:
The present invention relates, inter alia, to a process for preparing a compound of formula (I): using, as a catalyst 1,4-diazabicyclo[2.2.2]octane.
摘要:
The present invention relates, inter alia, to a process for preparing a compound of formula (I): which comprises either (a) reacting a compound of formula (II): with 2-cyanophenyl, or a salt thereof, in the presence of between 0.1 and 2 mol % of 1,4-diazabicyclo[2.2.2]octane, or (b) reacting a compound of the formula (III): with a compound of the formula (IV): in the presence of between 0.1 and 2 mol % of 1,4-diazabicyclo[2.2.2]octane; where W is the methyl (E)-2-(3-methoxy)acrylate group C(CO2CH3)═CHOCH3 or the methyl 2-(3,3-dimethoxy)propanoate group C(CO2CH3)CH(OCH3)2, or a mixture of the two groups. In addition, the present invention relates to a novel precursors of the compound of formula (I) and methods for making them.
摘要:
The present invention relates, inter alia, to a process for preparing a compound of formula (I): using a quinuclidine-based catalyst or an optionally 3-substituted N-methyl pryrrolidine-based catalyst.
摘要:
The present invention relates, inter alia, to a process for preparing a compound of formula (I): using a quinuclidine-based catalyst or an optionally 3-substituted N-methyl pryrrolidine-based catalyst.
摘要:
The present invention relates, inter alia, to a process for preparing a compound of formula (I): using, as a catalyst 1,4-diazabicyclo[2.2.2]octane.
摘要:
The present invention relates, inter alia, to a process for preparing a compound of formula (I): which comprises either (a) reacting a compound of formula (II): with 2-cyanophenyl, or a salt thereof, in the presence of between 0.1 and 2 mol % of 1,4-diazabicyclo[2.2.2]octane, or (b) reacting a compound of the formula (III): with a compound of the formula (IV): in the presence of between 0.1 and 2 mol % of 1,4-diazabicyclo[2.2.2]octane; where W is the methyl (E)-2-(3-methoxy)acrylate group C(CO2CH3)═CHOCH3 or the methyl 2-(3,3-dimethoxy)propanoate group C(CO2CH3)CH(OCH3)2, or a mixture of the two groups. In addition, the present invention relates to a novel precursors of the compound of formula (I) and methods for making them.
摘要:
Compounds of formula (1) ##STR1## are described wherein Y represents a halogen atom or a group --OR.sup.1, where R.sup.1 is an optionally substituted alkyl group; R.sup.2 represents an optionally substituted cycloalkyl or cycloalkenyl group; R.sup.3 is a monocyclic or bicyclic aryl group optionally containing one or more heteroatoms selected from oxygen or sulphur atoms or a group --N(R.sup.4)-- where R.sup.4 is a hydrogen atom or an alkyl group; X is --O--, --S--, or --N(R.sup.4)--, where R.sup.5 is a hydrogen or an alkyl group; with the proviso that when X is --O-- then R.sup.3 is not a 3-cyanamino-6-pyridazinyl or a 3-chloro-6-pyridazinyl group; and the salts, solvates, hydrates and N-oxides thereof. The compounds are selective and potent inhibitors of phosphodiesterase IV and are useful for the prophylaxis and treatment of inflammatory diseases and the alleviation of conditions associated with central nervous malfunction.
摘要:
Compounds of the general formula (1) ##STR1## are described wherein Y is halogen or --OR.sup.1, where R.sup.1 is optionally substituted alkyl; X is --O--, --S-- or --N(R.sup.8)-, where R.sup.8 is hydrogen or alkyl; R.sup.2 is optionally substituted alkyl, alkenyl, cycloalkyl or cycloalkenyl; R.sup.3 is hydrogen, halogen or --OR.sup.9, where R.sup.9 is hydrogen or optionally substituted alkyl, alkenyl, alkoxyalkyl, or alkanoyl, or formyl, carboxamido or thiocarboxamido; R.sup.4 is --(CH.sub.2).sub.n Ar, where Ar is monocyclic or bicyclic aryl optionally containing one or more heteroatoms selected from oxygen, sulfur and nitrogen atoms, wherein Ar is substituted by an optionally substituted C.sub.3-9 cycloaliphatic group optionally containing one or more heteroatoms selected from oxygen, sulphur or --N(R.sup.8)-, and n is zero or an integer 1, 2 or 3; R.sup.5 is --(CH.sub.2).sub.n Ar' where Ar' is monocyclic or bicyclic aryl optionally containing one or more heteroatoms selected from oxygen, sulfur or nitrogen atoms or is Ar; R.sup.6 is hydrogen or optionally substituted alkyl; and R.sup.7 is hydrogen or optionally substituted alkyl; or a salt, solvate or hydrate thereof. Compounds according to the invention are potent and selective phosphodiesterase type IV inhibitors and are useful in the prophylaxis and treatment of diseases such as asthma where an unwanted inflammatory response or muscular spasm is present.