Processes for the preparation of dolutegravir and pharmaceutically acceptable salts utilizing alkenylamine are disclosed. Intermediates in those synthetic schemes are also disclosed.

Processes for the preparation of dolutegravir and pharmaceutically acceptable salts utilizing alkenylamine are disclosed. Intermediates in those synthetic schemes are also disclosed.

The present invention relates to a process for the preparation of migalastat of formula (I) and intermediates useful in the synthesis thereof. The process comprises the reductive amination reaction of a compound of formula (VI).

##STR00001##

The present invention relates to a process for the preparation of migalastat of formula (I) and intermediates useful in the synthesis thereof. The process comprises the reductive amination reaction of a compound of formula (VI).

##STR00001##

An improved method is used for preparing triacetone amine while recycling the by-products. This involves treating the crude product from triacetone amine preparation, which leads to an increase in the content of compounds which react readily with ammonia. This method enables efficient recycling of the by-products formed in the synthesis of triacetone amine.

The present invention relates to kinetic resolution of racemic -hydroxyl ester via asymmetric catalytic hydrogenation and an application thereof. In the presence of chiral spiro pyridyl phosphine ligand Iridium catalyst and base, racemic -hydroxyl esters were subjected to asymmetric catalytic hydrogenation to obtain extent optical purity chiral -hydroxyl esters and corresponding 1,5-diols. An optically active chiral -hydroxyl ester and 1,5-diols can be obtained at very high enantioselectivity and yield with relatively low usage of catalyst. The chiral -hydroxyl ester and 1,5-diols obtained by using the method can be used as a critical raw material for asymmetric synthesis of chiral drugs (R)-lisofylline and natural drugs (+)-civet, ()-indolizidine 167B and ()-coniine.

The present invention relates to kinetic resolution of racemic -hydroxyl ester via asymmetric catalytic hydrogenation and an application thereof. In the presence of chiral spiro pyridyl phosphine ligand Iridium catalyst and base, racemic -hydroxyl esters were subjected to asymmetric catalytic hydrogenation to obtain extent optical purity chiral -hydroxyl esters and corresponding 1,5-diols. An optically active chiral -hydroxyl ester and 1,5-diols can be obtained at very high enantioselectivity and yield with relatively low usage of catalyst. The chiral -hydroxyl ester and 1,5-diols obtained by using the method can be used as a critical raw material for asymmetric synthesis of chiral drugs (R)-lisofylline and natural drugs (+)-civet, ()-indolizidine 167B and ()-coniine.

Enantioselective syntheses of cis- and trans-bicyclic dihydropyran compounds, and other intermediates, en route to heteroyohimbine alkaloids.

Enantioselective syntheses of cis- and trans-bicyclic dihydropyran compounds, and other intermediates, en route to heteroyohimbine alkaloids.

The invention relates to processes for preparing 2-(1-(tert-butoxycarbonyl)-piperidine-4-yl)benzoic acid having formula I: ##STR00001## Among its various uses, this compound is useful as an intermediate for preparing ampreloxetine and salts thereof.