The present invention describes thymoquinone compounds formula (I): (i) These compounds have been identified as being useful in the treatment of cancer. ##STR00001##

The present invention describes thymoquinone compounds formula (I): (i) These compounds have been identified as being useful in the treatment of cancer. ##STR00001##

The disclosure provides a method for synthesizing free base forms of (2R,6R)-hydroxynorketamine (HNK) and (2S,6S)-hydroxynorketamine. In an embodiment synthesis of (2R,6R)-hydroxynorketamine (HNK) includes preparation of (R)-norketamine via chiral resolution from racemic norketamine via a chiral resolution with L-pyroglutamic acid. The disclosure also provided crystal forms of the corresponding (2R,6R)-hydroxynorketamine (HNK) and (2S,6S)-hydroxynorketamine hydrochloride salts.

The disclosure provides a method for synthesizing free base forms of (2R,6R)-hydroxynorketamine (HNK) and (2S,6S)-hydroxynorketamine. In an embodiment synthesis of (2R,6R)-hydroxynorketamine (HNK) includes preparation of (R)-norketamine via chiral resolution from racemic norketamine via a chiral resolution with L-pyroglutamic acid. The disclosure also provided crystal forms of the corresponding (2R,6R)-hydroxynorketamine (HNK) and (2S,6S)-hydroxynorketamine hydrochloride salts.

The disclosure provides a method for synthesizing free base forms of (2R,6R)-hydroxynorketamine (HNK) and (2S,6S)-hydroxynorketamine. In an embodiment synthesis of (2R,6R)-hydroxynorketamine (HNK) includes preparation of (R)-norketamine via chiral resolution from racemic norketamine via a chiral resolution with L-pyroglutamic acid. The disclosure also provided crystal forms of the corresponding (2R,6R)-hydroxynorketamine (HNK) and (2S,6S)-hydroxynorketamine hydrochloride salts.

The present application provides a preparation method of a formamide compound, the preparation process includes: uniformly mixing raw material of methanoic acid and an amine compound selected from a primary amine or a secondary amine to prepare a homogeneous reaction system; the above homogeneous reaction system is heated to 160-230 C., allowing carbon monoxide to be decomposed from the homogeneous reaction system and participates in the reaction, and collecting the reaction product to obtain a formamide compound. The present application provides a new technology using a homogeneous method to synthesize a formamide compound, the reaction process needs no use of a catalyst, the operation process is simple and controllable, and the raw material of the amine compound has a high selectivity.

The present application provides a preparation method of a formamide compound, the preparation process includes: uniformly mixing raw material of methanoic acid and an amine compound selected from a primary amine or a secondary amine to prepare a homogeneous reaction system; the above homogeneous reaction system is heated to 160-230 C., allowing carbon monoxide to be decomposed from the homogeneous reaction system and participates in the reaction, and collecting the reaction product to obtain a formamide compound. The present application provides a new technology using a homogeneous method to synthesize a formamide compound, the reaction process needs no use of a catalyst, the operation process is simple and controllable, and the raw material of the amine compound has a high selectivity.

The invention relates to a process for preparation of the compound 3-methyl-5-benzyloxy-2-(4-benzyloxyphenyl)-1H-indole 5, an intermediate for the synthesis of bazedoxifene and bazedoxifene acetate. ##STR00001##

The invention relates to a process for preparation of the compound 3-methyl-5-benzyloxy-2-(4-benzyloxyphenyl)-1H-indole 5, an intermediate for the synthesis of bazedoxifene and bazedoxifene acetate. ##STR00001##

The present invention relates to new methods of manufacturing benzoquinoline inhibitors of vesicular monoamine transporter 2 (VMAT2), and intermediates thereof.

##STR00001##