摘要:
The instant invention concerns processes for the production of pyrrole-2-carbonitriles such as 1-methylpyrrole-2-carbonitrile. Such processes preferably comprise the steps of reacting a pyrrole with chlorosulfonyl isocyanate in the presence of a solvent and contacting the resulting product with a molar excess of an amide such as N,N-dimethylformamide. The product of this contacting step is then contacted with a molar excess of an organic base to produce a precipitate and a solution phase. The precipitate is then separated from the solution phase and the corresponding pyrrole-2-carbonitrile is isolated from the resulting solution phase.
摘要:
Methods for purifying a compound of formula I are provided, wherein A, B X, Q, and R1 are defined herein. The methods include mixing the compound of formula I and a solvent; adding a base to the solvent; and precipitating purified compound of formula I.
摘要:
Micronized tanaproget, purified tanaproget Form I, and micronized, purified tanaproget Form I are provided. Also provided are compositions containing one or more of the prepared tanaproget forms, methods of using one or more of the prepared tanaproget forms, and kits containing one or more of the prepared tanaproget forms.
摘要翻译:提供微粉化的钠盐瓶,纯化的tanaproget Form I和微粉化的纯化的Tanaproget Form I。 还提供了含有一种或多种所制备的钛酸钠形式的组合物,使用一种或多种所制备的钛酸钠形式的方法,以及包含一种或多种所制备的钛酸钠形式的试剂盒。
摘要:
A convenient preparation of boron-containing compounds, borate salts, pyrrolecarbonitrile boron-containing compounds, N-substituted-pyrrole-2-carbonitrile boron-containing compounds, and derivatives thereof is provided. The present invention also provides for the use of these boron-containing compounds and derivatives thereof in coupling reactions to provide bi-aryl compounds.
摘要:
Processes for preparing amino alcohols or salts thereof and sulfonamide substituted alcohol compounds are provided. Desirably, the sulfonamide substituted alcohol compounds are heterocyclic sulfonamide trifluoroalkyl-substituted alcohol compounds or phenyl sulfonamide trifluoroalkyl-substituted alcohol compounds.
摘要:
Processes for preparing amino alcohols or salts thereof and sulfonamide substituted alcohol compounds are provided. Desirably, the sulfonamide substituted alcohol compounds are heterocyclic sulfonamide trifluoroalkyl-substituted alcohol compounds or phenyl sulfonamide trifluoroalkyl-substituted alcohol compounds.
摘要:
There is provided a process for the preparation of substituted amino alcohols HO—(CH2)n—NR1R2 from haloalcohols HO—(CH2)n—X, where X is Cl, Br or I, by reaction with an amine HNR1R2, in water as solvent at a temperature range of about 20° C. to about 90° C. optionally in the presence of a catalytic amount of an iodide source metal iodides. The haloalcohols are useful in the preparation of 6-[(substituted)phenyl]-triazolopyrimidine compounds which are useful in the treatment of cancer.
摘要:
There is provided a process for the preparation of substituted amino alcohols HO—(CH2)n—NR1R2 from haloalcohols HO—(CH2)n—X, where X is Cl, Br or I, by reaction with an amine HNR1R2, in water as solvent at a temperature range of about 20° C. to about 90° C. optionally in the presence of a catalytic amount of an iodide source metal iodides. The haloalcohols are useful in the preparation of 6-[(substituted)phenyl]-triazolopyrimidine compounds which are useful in the treatment of cancer.
摘要翻译:提供了用于制备取代的氨基醇HO-(CH 2)n - NR 1 - , - O 2的方法, 其中X是Cl,Br或I,通过与胺HNR 1反应而得到的卤代醇HO-(CH 2)n -X 在约20℃至约90℃的温度范围内的水溶液中,任选地在催化量的碘化物源金属碘化物的存在下进行。 卤代醇可用于制备可用于治疗癌症的6 - [(取代的)苯基] - 三唑并嘧啶化合物。