C07D211/74

Intermediates for optically active piperidine derivatives and preparation methods thereof

A preparation method according to the present invention makes it possible to industrially produce large amounts of highly pure optically active tert-butyl 3-methyl-4-oxopiperidine-1-carboxylate in high yield by use of commercially available reagents and solvents. In addition, the use of novel intermediates according to the present invention makes it possible to produce highly pure optically active tert-butyl 3-methyl-4-oxopiperidine-1-carboxylate in high yield.

Intermediates for optically active piperidine derivatives and preparation methods thereof

A preparation method according to the present invention makes it possible to industrially produce large amounts of highly pure optically active tert-butyl 3-methyl-4-oxopiperidine-1-carboxylate in high yield by use of commercially available reagents and solvents. In addition, the use of novel intermediates according to the present invention makes it possible to produce highly pure optically active tert-butyl 3-methyl-4-oxopiperidine-1-carboxylate in high yield.

A PROCESS FOR SYNTHESIS OF PIPERIDINE ALKALOIDS
20170267636 · 2017-09-21 ·

The present invention discloses a process for synthesis of piperidine alkaloids selected from fagomine, 4-epi-fagomine and nojirimycin from tri-O-benzyl-D-glucal or tri-O-benzyl-D-galactal.

A PROCESS FOR SYNTHESIS OF PIPERIDINE ALKALOIDS
20170267636 · 2017-09-21 ·

The present invention discloses a process for synthesis of piperidine alkaloids selected from fagomine, 4-epi-fagomine and nojirimycin from tri-O-benzyl-D-glucal or tri-O-benzyl-D-galactal.

METHODS OF MANUFACTURING OF NIRAPARIB

Disclosed herein are methods and processes of preparing niraparib and pharmaceutically acceptable salts thereof, and intermediates and their salts useful for the synthesis of niraparib.

HETEROGENEOUS CATALYZED PROCESS FOR THE PRODUCTION OF 2,2,6,6-TETRAMETHYL-4-PIPERIDONE

The present invention relates to a process for the production of 2,2,6,6-tetramethyl-4-piperidone particularly comprising (i) providing a reactor containing a catalyst comprising a zeolitic material having a framework structure of FAU, wherein the zeolitic material comprises YO.sub.2 and X.sub.2O.sub.3 in its framework structure, wherein Y is a tetravalent element and X is a trivalent element, wherein the zeolitic material has an YO.sub.2 to X.sub.2O.sub.3 molar ratio of 16 to 175; (ii) preparing a reaction mixture comprising acetone and ammonia; (iii) contacting the catalyst in the reactor with the reaction mixture prepared in (ii) at a temperature in the range of from 40 to 250° C. for obtaining a reaction product comprising 2,2,6,6-tetramethyl-4-piperidone;
wherein the mixture prepared in (ii) and contacted with the catalyst in (iii) contains less than 10 weight-% of water based on 100 weight-% of the reaction mixture.

HETEROGENEOUS CATALYZED PROCESS FOR THE PRODUCTION OF 2,2,6,6-TETRAMETHYL-4-PIPERIDONE

The present invention relates to a process for the production of 2,2,6,6-tetramethyl-4-piperidone particularly comprising (i) providing a reactor containing a catalyst comprising a zeolitic material having a framework structure of FAU, wherein the zeolitic material comprises YO.sub.2 and X.sub.2O.sub.3 in its framework structure, wherein Y is a tetravalent element and X is a trivalent element, wherein the zeolitic material has an YO.sub.2 to X.sub.2O.sub.3 molar ratio of 16 to 175; (ii) preparing a reaction mixture comprising acetone and ammonia; (iii) contacting the catalyst in the reactor with the reaction mixture prepared in (ii) at a temperature in the range of from 40 to 250° C. for obtaining a reaction product comprising 2,2,6,6-tetramethyl-4-piperidone;
wherein the mixture prepared in (ii) and contacted with the catalyst in (iii) contains less than 10 weight-% of water based on 100 weight-% of the reaction mixture.

Chemical process for preparing phenylpiperidinyl indole derivatives

The present invention relates to a method of synthesizing a compound of formula (I) also referred to as 4-((2S,4S)-(4-ethoxy-1-((5-methoxy-7-methyl-1H-indol-4-yl)methyl)piperidin-2-yl))benzoic acid, or a pharmaceutically acceptable salt thereof, and/or intermediates thereof, their use as pharmaceuticals and pharmaceutical compositions and the use of intermediates for preparing a compound of formula (I), or a pharmaceutically acceptable salt thereof.

Chemical process for preparing phenylpiperidinyl indole derivatives

The present invention relates to a method of synthesizing a compound of formula (I) also referred to as 4-((2S,4S)-(4-ethoxy-1-((5-methoxy-7-methyl-1H-indol-4-yl)methyl)piperidin-2-yl))benzoic acid, or a pharmaceutically acceptable salt thereof, and/or intermediates thereof, their use as pharmaceuticals and pharmaceutical compositions and the use of intermediates for preparing a compound of formula (I), or a pharmaceutically acceptable salt thereof.

Alzheimer's Disease Assay in a Living Patient

An assay for Alzheimer's disease pathology (AD) in a living patient is disclosed wherein an amount of α7nAChR or TLR4 in a FLNA-captured protein complex or α7nAChR in an Aβ-captured protein complex or α7nAChR-FLNA, TLR4-FLNA and/or α7nAChR-Aβ.sub.42 complex present as a protein-protein complex in a sample is determined and compared to the amount in a standard sample from a person free of AD pathology. An amount greater than in the standard sample indicates AD pathology. Also disclosed is an assay predictive of prognosis for treatment with a medicament in which the amount of an above protein or protein complex is determined and compared to an amount determined in the presence of a medicament that binds to a FLNA pentapeptide and contains at least four of the six pharmacophores of FIGS. 7-12. An amount of protein or protein complex determined in the presence of the medicament less than the first determined amount indicates a favorable treatment prognosis.