C07C211/29

Metallorganocatalysis for asymmetric transformations

A ligand having the structure or its enantiomer; (I) wherein: each one of R.sub.a, R.sub.b, R.sub.c and R.sub.d is selected from alkyl, cycloalkyl, and aryl; the bridge group is selected from CH.sub.2NH; *CH(CH.sub.3)NH(C*,R); and the organocatalyst is an organic molecule catalyst covalently bound to the bridge group. Also, a catalyst having the structure or its enantiomer: (II) wherein: each one of R.sub.a, R.sub.b, R.sub.c and R.sub.d is selected from alkyl, cycloalkyl, and aryl; the bridge group is selected from CH.sub.2NH; *CH(CH.sub.3)NH(C*,R); and *CH(CH.sub.3)NH(C*,S); the organocatalyst is an organic molecule catalyst covalently bound to the bridge group; and M is selected from the group consisting of Rh, Pd, Cu, Ru, Ir, Ag, Au, Zn, Ni, Co, and Fe. ##STR00001##

PROCESS FOR THE SYNTHESIS OF (+) AND (-)-1-(3,4-DICHLOROPHENYL)-3-AZABICYCLO[3.1.0]HEXANE
20170233333 · 2017-08-17 ·

The present invention is concerned with novel processes for the preparation of (+)-1-(3,4-dichlorophenyl)-3-azabicyclo[3.1.0]hexane or a pharmaceutically acceptable salt thereof, and (−)-1-(3,4-dichlorophenyl)-3-azabicyclo[3.1.0]hexane or a pharmaceutically acceptable salt thereof. These compounds have pharmaceutical utility and are known to be useful for treating e.g., depression, anxiety disorders, eating disorders and urinary incontinence.

PROCESS FOR THE SYNTHESIS OF (+) AND (-)-1-(3,4-DICHLOROPHENYL)-3-AZABICYCLO[3.1.0]HEXANE
20170233333 · 2017-08-17 ·

The present invention is concerned with novel processes for the preparation of (+)-1-(3,4-dichlorophenyl)-3-azabicyclo[3.1.0]hexane or a pharmaceutically acceptable salt thereof, and (−)-1-(3,4-dichlorophenyl)-3-azabicyclo[3.1.0]hexane or a pharmaceutically acceptable salt thereof. These compounds have pharmaceutical utility and are known to be useful for treating e.g., depression, anxiety disorders, eating disorders and urinary incontinence.

IMPROVED PROCESS FOR THE REDUCTIVE AMINATION OF HALOGEN-CONTAINING SUBSTRATES

Disclosed is a process for performing a reductive amination of a first functional group in an organic feed substrate, which feed substrate comprises at least one further functional group containing a halogen atom, wherein the halogen atom is selected from the list consisting of chlorine, bromine, iodine, and combinations thereof, in the presence of hydrogen and a heterogeneous catalyst comprising at least one metal from the list of Pd, Pt, Rh, Ir, and Ru, and in absence of any catalytic amount of any second metal from the list consisting of Ag, Ni, Co, Sn, Bi, Cu, Au, and combinations thereof. The process is preferably applied for the reductive amination of 2-chloro-benzaldehyde to form 2-chloro-benzyldimethylamine, as an intermediate in the production of active agrochemical compounds and microbicides of the methoximinophenylglyoxylic ester series.

IMPROVED PROCESS FOR THE REDUCTIVE AMINATION OF HALOGEN-CONTAINING SUBSTRATES

Disclosed is a process for performing a reductive amination of a first functional group in an organic feed substrate, which feed substrate comprises at least one further functional group containing a halogen atom, wherein the halogen atom is selected from the list consisting of chlorine, bromine, iodine, and combinations thereof, in the presence of hydrogen and a heterogeneous catalyst comprising at least one metal from the list of Pd, Pt, Rh, Ir, and Ru, and in absence of any catalytic amount of any second metal from the list consisting of Ag, Ni, Co, Sn, Bi, Cu, Au, and combinations thereof. The process is preferably applied for the reductive amination of 2-chloro-benzaldehyde to form 2-chloro-benzyldimethylamine, as an intermediate in the production of active agrochemical compounds and microbicides of the methoximinophenylglyoxylic ester series.

Metabolism resistant fenfluramine analogs and methods of using the same

Metabolism-resistant fenfluramine analogs are provided. The subject fenfluramine analogs find use in the treatment of a variety of diseases. For example, methods of treating epilepsy by administering a fenfluramine analog to a subject in need thereof are provided. Also provided are methods of suppressing appetite in a subject in need thereof. Pharmaceutical compositions for use in practicing the subject methods are also provided.

Metabolism resistant fenfluramine analogs and methods of using the same

Metabolism-resistant fenfluramine analogs are provided. The subject fenfluramine analogs find use in the treatment of a variety of diseases. For example, methods of treating epilepsy by administering a fenfluramine analog to a subject in need thereof are provided. Also provided are methods of suppressing appetite in a subject in need thereof. Pharmaceutical compositions for use in practicing the subject methods are also provided.

PROCESS FOR PREPARATION OF HALOGENATED BENZYLAMINE AND INTERMEDIATES THEROF

The present invention provides an improved process for the preparation of halogenated benzylamine having the formula I from halogenated benzonitriles, Formula I wherein, X.sub.1 is selected from group consisting of hydrogen, chloro or fluoro, provided at least one X.sub.1 is chloro or fluoro.

##STR00001##

PROCESS FOR PREPARATION OF HALOGENATED BENZYLAMINE AND INTERMEDIATES THEROF

The present invention provides an improved process for the preparation of halogenated benzylamine having the formula I from halogenated benzonitriles, Formula I wherein, X.sub.1 is selected from group consisting of hydrogen, chloro or fluoro, provided at least one X.sub.1 is chloro or fluoro.

##STR00001##

Method for efficiently synthesizing primary amines

Disclosed is a method for efficiently synthesizing primary amines, which comprises using carbonyl compounds or alcohol compounds as reaction substrate, liquid ammonia or alcohol solutions of ammonia as nitrogen source, and hydrogen as hydrogen source, and reacting in reaction medium catalyzed by a cobalt-based catalyst to obtain the primary amines. Due to high catalytic activity, the method can realize the reductive amination of carbonyl compounds and the hydrogen-borrowing amination of alcohol compounds at low temperatures in a short time to obtain the primary amines with high yield, and is applicable to a wide range of substrates. The obtained primary amines can be used as raw materials with high extra value for producing polymers, medicines, dyes and surfactants. Further, the cobalt-based catalyst has a good industrial application prospect because it is magnetic which can facilitate separation and recycling of the catalyst. Moreover, the inexpensive cobalt-based catalyst can significantly reduce industrialization cost.