C07C201/14

METHOD FOR THE SYNTHESIS OF 2,4-DIMETHYLPYRIMIDIN-5-OL, INTERMEDIATES, AND METHOD FOR THE SYNTHESIS OF LEMBOREXANT USING THE INTERMEDIATES
20230092143 · 2023-03-23 ·

A method is for the synthesis of 2,4-dimethylpyrimidin-5-ol, which can be used as an intermediate compound in the synthesis of Lemborexant. The method includes reacting a nitrophenyl compound with N,N-dimethylformamide diethyl acetal.

METHOD FOR THE SYNTHESIS OF 2,4-DIMETHYLPYRIMIDIN-5-OL, INTERMEDIATES, AND METHOD FOR THE SYNTHESIS OF LEMBOREXANT USING THE INTERMEDIATES
20230092143 · 2023-03-23 ·

A method is for the synthesis of 2,4-dimethylpyrimidin-5-ol, which can be used as an intermediate compound in the synthesis of Lemborexant. The method includes reacting a nitrophenyl compound with N,N-dimethylformamide diethyl acetal.

Process for the halogenation at the alpha-h position of alkylarenes variously substituted on the aromatic ring

A process that allows halogenation at the alpha-H position of alkylarenes, optionally further substituted on the aromatic or heteroaromatic ring, is described.

Process for the halogenation at the alpha-h position of alkylarenes variously substituted on the aromatic ring

A process that allows halogenation at the alpha-H position of alkylarenes, optionally further substituted on the aromatic or heteroaromatic ring, is described.

PROCESS FOR THE HALOGENATION AT THE ALPHA-H POSITION OF ALKYLARENES VARIOUSLY SUBSTITUTED ON THE AROMATIC RING

A process that allows halogenation at the alpha-H position of alkylarenes, optionally further substituted on the aromatic or heteroaromatic ring, is described.

PROCESS FOR THE HALOGENATION AT THE ALPHA-H POSITION OF ALKYLARENES VARIOUSLY SUBSTITUTED ON THE AROMATIC RING

A process that allows halogenation at the alpha-H position of alkylarenes, optionally further substituted on the aromatic or heteroaromatic ring, is described.

Synthesis of desosamines

The present invention provides desosamine and mycaminose analogs and nitro sugars and methods for their preparation. The invention also provides methods of cyclizing a compound of Formula (A′) with glyoxal to give a nitro sugar of Formula (B). Methods for the preparation of compound of Formula (D′) are provided comprising cyclization of a nitro alcohol to give a nitro sugar and reduction and alkylation of the nitro sugar to give a desosamine, mycaminose, or an analog thereof. ##STR00001##

Synthesis of desosamines

The present invention provides desosamine and mycaminose analogs and nitro sugars and methods for their preparation. The invention also provides methods of cyclizing a compound of Formula (A′) with glyoxal to give a nitro sugar of Formula (B). Methods for the preparation of compound of Formula (D′) are provided comprising cyclization of a nitro alcohol to give a nitro sugar and reduction and alkylation of the nitro sugar to give a desosamine, mycaminose, or an analog thereof. ##STR00001##

SELECTIVE INHIBITORS OF NLRP3 INFLAMMASOME

The present disclosure relates to compounds of Formula (I):

##STR00001##

and to their pharmaceutically acceptable salts, pharmaceutical compositions, methods of use, and methods for their preparation. The compounds disclosed herein are useful for inhibiting the maturation of cytokines of the IL-1 family by inhibiting inflammasomes and may be used in the treatment of disorders in which inflammasome activity is implicated, such as autoinflammatory and autoimmune diseases and cancers.

SELECTIVE INHIBITORS OF NLRP3 INFLAMMASOME

The present disclosure relates to compounds of Formula (I):

##STR00001##

and to their pharmaceutically acceptable salts, pharmaceutical compositions, methods of use, and methods for their preparation. The compounds disclosed herein are useful for inhibiting the maturation of cytokines of the IL-1 family by inhibiting inflammasomes and may be used in the treatment of disorders in which inflammasome activity is implicated, such as autoinflammatory and autoimmune diseases and cancers.