Centre National De La Recherche Scientifique

Universitè De Montpellier

Ecole Nationale Superieure De Chimie De Montpellier

Association Pour La Recherche Et Le Developpement Des Methodes Et Processus Industriels

Instytut Farmakologii Polskiej Akademii Nauk

Ecole Des Mines D'ales

Uniwersyter Jagiellonski

Centre National De La Recherche Scientifique-cnrs

Uniwersytet Jagiellonski

Université De Montpellier I

Frédéric Lamaty

Jean Martinez

Gilles Subra

Maciej Pawlowski

Pawel Zajdel

Grzegorz Satala

Andrzej J Bojarski

Anna Wesolowska

Piotr Popik

Tomasz Kos

Anna Partyka

Evelina Colacino

Xavier Bantreil

Katarzyna Grychowska

Valérie Declerck

Benjamin Gallard

Yves Yeboue

Nicolas Le Moigne

Thomas-Xavier Metro

Wesolowska Anna

A continuous, solvent-free and non-enzymatic method for synthesizing a compound of formula (I): Ra-POLYPEP-Rc (I) wherein: POLYPEP is a poly-amino acid compound, Ra and Rc are as specified, the method including the steps of: a) feeding an extrusion reactor with (1) a compound of formula (II) Ra-PEPNt-Rg (II) wherein; PEPNt is a mono- or a poly-amino acid compound, Ra and Rg are as specified, and (2) a compound of formula (III) H-PEPCt-Rc (III) wherein: PEPCt is a mono- or a poly-amino acid compound, and Rc is as defined in the absence of any solvent, so that the compound of formula (II) and the compound of formula (III) react together for generating a compound of formula (I), and b) collecting the compound of formula (I) from the extrusion reactor.

Continuous, solvent-free and non-enzymatic peptide synthesis by reactive extrusion

This invention concerns pyrroloquinoline derivatives as antagonists of 5-HT6 receptors, to methods for the preparation of these compounds and to novel intermediates useful for their synthesis. The invention also relates to the uses of such compounds and compositions, particularly their use in administering them to patients to achieve a therapeutic effect in schizophrenia, anxiety, depression, maniac depression, epilepsy, obsessive compulsive disorders, mood disorders, migraine, Alzheimer's disease, age related cognitive decline, mild cognitive impairment, sleep disorders, eating disorders, anorexia, bulimia, panic attacks, attention deficit hyperactivity disorder, attention deficit disorder, Parkinson's disease, Huntington's disease, withdrawal from abuse of cocaine, ethanol, nicotine or benzodiazepines, pain, obesity and type-2 diabetes, functional bowel disorder, Irritable Bowel Syndrome. The compounds have the general formula (XIV), wherein the symbols have the meanings given in the description.

[object Object]

The disclosure relates to a method for the synthesis of a compound of the formula (I) in which: n is an integer higher than or equal to 1; Rb and each Rn are independently a hydrogen atom, a C-Carylalkyl group or a C-Calkyl group substituted or not by an aryl group, &#x2014;COOH, C-C, &#x2014;COO-(alkyl), &#x2014;CONH, &#x2014;SH, heteroaryl, &#x2014;NH, &#x2014;NHC(NH)(NH), C-C-s-(alkyl), &#x2014;OH or phenol; Ra is a N-protective group; Rc is a ORd group in which Rd is a C-Calkyl group or a NReRf group in which Re and Rf Re independently an N-protective group.

Method for the synthesis of peptides without solvent

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Montpellier, France

Frédéric Lamaty