摘要:
The present invention relates to an improved process for the in situ preparation of diisopinocampheylchloroborane which comprises reacting sodium borohydride and boron trichloride with .alpha.-pinene. The diisopinocampheylchloroborane thus obtained may be used, without isolation, to reduce prochiral ketones to their corresponding alcohols in high optical purity.
摘要翻译:本发明涉及一种二异蒎烷基氯代硼烷的原位制备改进方法,其包括使硼氢化钠和三氯化硼与α-蒎烯反应。 这样得到的二蒎烯yl yl chlor chlor ob or or may。。。。。。。,,,。。。。。。。。。。。。。
摘要:
The present invention relates to an improved process for the in situ preparation of diisopinocampheylchloroborane which comprises reacting sodium borohydride and boron trichloride with .alpha.-pinene. The diisopinocampheylchloroborane thus obtained may be used, without isolation, to reduce prochiral ketones to their corresponding alcohols in high optical purity.
摘要翻译:本发明涉及一种二异蒎烷基氯代硼烷的原位制备改进方法,其包括使硼氢化钠和三氯化硼与α-蒎烯反应。 这样得到的二蒎烯yl yl chlor chlor ob or or may。。。。。。。,,,。。。。。。。。。。。。。
摘要:
The bisulfate salt of N,N-dimethyl-2-�5-(1,2,4-triazol-1-ylmethyl)-1H-indol-3-yl!ethylamine is a selective agonist of 5-HT.sub.1 -like receptors and is useful in the treatment of migraine and associated disorders.
摘要:
A new process is described for the synthesis of the triazolyl tryptamine: ##STR1## and related compounds. The process involves a palladium-catalyzed ring closure between a substituted ortho-iodoaniline and a protected 1-alkynol. The process is carded out at high temperature, e.g. 100.degree. C., in a dry inert solvent, e.g., DMF and in the presence of a proton acceptor, e.g., Na.sub.2 CO.sub.3 or a trialkylamine. The triazolyl tryptamine, as well as acid addition salts thereof, is a 5 HT.sub.1 D receptor agonist having anti-migraine properties.
摘要翻译:描述了三唑基色胺的合成的新方法:< IMAGE>和相关化合物。 该方法涉及取代的邻碘苯胺和被保护的1-炔醇之间的钯催化的闭环。 该过程在高温下梳理,例如 在干惰性溶剂如DMF中并在质子受体例如Na 2 CO 3或三烷基胺存在下进行。 三唑基色胺及其酸加成盐是具有抗偏头痛性质的5 HT1D受体激动剂。
摘要:
Polymorphic forms of the angiotensin II receptor antagonist, 3-�2'-(N-benzoyl)sulfonamidobiphenyl-4-yl!methyl-5,7-dimethyl-2-ethyl-3H-imidazo�4,5-b!pyridine and a method for the preparation of these crystal forms.
摘要:
This invention relates to a method for the preparation of a compound of formula I: ##STR1## a key intermediate in the synthesis of a series of Angiotensin II receptor antagonists. The invention also relates to a selective reagent for conducting the Hofmann rearrangement, particularly in the formation of a pyridinoimidazolone, which is a percursor to the formation of an imidazopyfidine of formula I. This invention also relates to a method for the preparation of imidazolutidine, a key intermediate in the synthesis of 3-(2'-(N-benzoyl)sulfonamidobiphen-4-yl)-methyl-5,7 -dimethyl-2-ethyl-3H-imidazo[4,5-b]pyridine, using pyridinoimidazolone, an unreactive urea.
摘要:
.beta.- or .gamma.-Ketoesters and .beta.- or .gamma.-ketoamides are asymmetrically reduced with a Ru(II)-BINAP derived catalyst at about 40.degree. C. and about 50 N/mm.sup.2 of hydrogen in the presence of a strong acid.
摘要翻译:在强酸存在下,在约40℃和约50N / mm 2的氢气下使用Ru(II)-BINAP衍生的催化剂不对称地还原β-或γ-甲酯和β-酮酰胺。
摘要:
A process of synthesizing a compound of the formula 1: ##STR1## is disclosed, which comprises reacting a compound of the formula 2: ##STR2## with diphenylphosphine in the presence of an amine base and a nickel catalyst to produce a compound of formula 1.
摘要:
A novel acylation process using an alkali metal bromide and a dialkylaminopyridine to form a sterically hindered ester functionality from an alkanoyl chloride and an alcohol is disclosed.
摘要:
A novel hydrogenation process, using a homogenous iridium or rhodium catalyst for selectively adding hydrogen to the 3,5 positions in the polyhydronaphthyl ring of lovastatin, simvastatin or C-8-acyl or C-6-substituted analogs thereof, is disclosed.