C07C53/134

PROCESS AND INTERMEDIATE
20200283374 · 2020-09-10 · ·

Process for the preparation of a compound of Formula (I):

##STR00001## the process comprising the reaction of a compound of Formula (II) with malononitrile in the presence of a base and a palladium catalyst,

##STR00002## wherein X, Y and Z, independently of each other, represent fluoro, chloro or C.sub.1-4alkyl; and L is a leaving group; with the proviso that 1 or 2 of X and Y are, independently of each other, fluoro or chloro.

PROCESS AND INTERMEDIATE
20200283374 · 2020-09-10 · ·

Process for the preparation of a compound of Formula (I):

##STR00001## the process comprising the reaction of a compound of Formula (II) with malononitrile in the presence of a base and a palladium catalyst,

##STR00002## wherein X, Y and Z, independently of each other, represent fluoro, chloro or C.sub.1-4alkyl; and L is a leaving group; with the proviso that 1 or 2 of X and Y are, independently of each other, fluoro or chloro.

Process for the preparation of phenylmalonic acid dinitriles

Process for the preparation of a compound of Formula (I), the process comprising the reaction of a compound of Formula (II) with malononitrile in the presence of a base and a palladium catalyst, Formula (II) wherein X, Y and Z, independently of each other, represent fluoro, chloro or C.sub.1-4alkyl; and L is a leaving group; with the proviso that 1 or 2 of X and Y are, independently of each other, fluoro or chloro. ##STR00001##

Process for the preparation of phenylmalonic acid dinitriles

Process for the preparation of a compound of Formula (I), the process comprising the reaction of a compound of Formula (II) with malononitrile in the presence of a base and a palladium catalyst, Formula (II) wherein X, Y and Z, independently of each other, represent fluoro, chloro or C.sub.1-4alkyl; and L is a leaving group; with the proviso that 1 or 2 of X and Y are, independently of each other, fluoro or chloro. ##STR00001##

Synthesis of terphenyl compounds

The present invention relates novel methods of synthesizing terphenyl compounds and in particular to novel methods for the synthesis of a compound of Formula I or intermediates thereof. ##STR00001##

Synthesis of terphenyl compounds

The present invention relates novel methods of synthesizing terphenyl compounds and in particular to novel methods for the synthesis of a compound of Formula I or intermediates thereof. ##STR00001##

HIGHLY ACCURATE DE NOVO POLYNUCLEOTIDE SYNTHESIS
20200222875 · 2020-07-16 ·

Methods, systems, compositions, and devices for the manufacturing of high-quality building blocks, such as polynucleotides, are described herein. Processes described herein provide for efficient washing of residual reagents, solvents, or byproducts from previous synthetic steps to allow for the generation of polynucleotides with low error rates. Processes described herein also provide for reduction in deletion rates during chemical nucleic acid synthesis. Further, methods and devices described herein allow for the rapid construction and assembly of large libraries of highly accurate polynucleotides.

PKC-activating compounds for the treatment of neurodegenerative diseases

The present invention relates to methods of activate an isoform of protein kinase C (PKC) for the treatment of neurological diseases including Alzheimer's disease and stroke using cyclopropanated or epoxidized derivatives of mono- and polyunsaturated fatty acids. The present invention also relates to methods of reducing neurodegeneration using cyclopropanated or epoxidized derivatives of mono- and polyunsaturated fatty acids.

PKC-activating compounds for the treatment of neurodegenerative diseases

The present invention relates to methods of activate an isoform of protein kinase C (PKC) for the treatment of neurological diseases including Alzheimer's disease and stroke using cyclopropanated or epoxidized derivatives of mono- and polyunsaturated fatty acids. The present invention also relates to methods of reducing neurodegeneration using cyclopropanated or epoxidized derivatives of mono- and polyunsaturated fatty acids.

SUBSTITUTED AROMATIC COMPOUNDS AND RELATED METHOD FOR THE TREATMENT OF FIBROSIS

The present invention relates to compounds of:

##STR00001##

or a pharmaceutically acceptable salt thereof, wherein

A is O.sub.5 alkyl, C.sub.6 alkyl, C.sub.5 alkenyl, C.sub.6 alkenyl, C(O)(CH.sub.2).sub.nCH.sub.3 or CH(OH)(CH.sub.2).sub.nCH.sub.3 wherein n is 3 or 4;

R.sub.1 is H, F or OH;

R.sub.2 is C.sub.5 alkyl, C.sub.6 alkyl, C.sub.5 alkenyl, C.sub.6 alkenyl, C(O)(CH.sub.2).sub.nCH.sub.3 or CH(OH)(CH.sub.2).sub.nCH.sub.3 wherein n is 3 or 4;

R.sub.3 is H, F, OH or CH.sub.2Ph;

R.sub.4 is H, F or OH;

Q is 1) (CH.sub.2).sub.mC(O)OH wherein m is 1 or 2, 2) CH(CH.sub.3)C(O)OH, 3) C(CH.sub.3).sub.2C(O)OH, 4) CH(F)C(O)OH, 5) CF.sub.2C(O)OH, or 6) C(O)C(O)OH;

and compositions comprising the same and the method using the same for the prevention or treatment of various fibrotic diseases and conditions in subjects, including pulmonary fibrosis, liver fibrosis, skin fibrosis, renal fibrosis, pancreas fibrosis, systemic sclerosis, cardiac fibrosis or macular degeneration.