Abstract: Subject-matter of the invention is a process for the preparation of a key intermediate in the synthesis of indacaterol. Subject-matter of the invention are also new synthesis intermediates.
Abstract: Disclosed is a process for the preparation of Enzalutamide comprising the reaction (Scheme 2), wherein R can be alkyl, aryl, aryl-alkyl or heterocyclyl.
Abstract: The present invention refers to a process for the preparation of 1-(2-halogen-ethyl)-4-piperidinecarboxylic acid ethyl esters, in particular of 1-(2-chloroethyl)-4 piperidinecarboxylic acid ethyl ester, a versatile synthesis intermediate, particularly useful as an intermediate compound in the synthesis of umeclidinium.
Abstract: Disclosed is an efficient method of synthesising Enzalutamide, which comprises the cyclisation reaction of isothiocyanate 1 with acid 3 pre-treated with a silylating agent, or reacting 1 and 3 in the presence of a silylating agent.
Type:
Application
Filed:
May 24, 2016
Publication date:
May 31, 2018
Applicant:
Olon S.P.A.
Inventors:
Samuele Frigoli, Davide Longoni, Marco Alpegiani
Abstract: Disclosed is a process for the preparation of Enzalutamide comprising the reaction (Scheme 2), wherein R can be alkyl, aryl, aryl-alkyl or heterocyclyl.
Abstract: Disclosed is a process for the synthesis of the active ingredients ospemifene and fispemifene which comprises reacting phenol 4 with an alkylating agent X—CH2CH2—Y of formula 7, wherein X is a leaving group and Y is the —(OCH2CH2)nOH group wherein n is zero or 1; or X and Y, taken together, represent an oxygen atom; to give ospemifene or fispemifene of formula 8.
Abstract: The present invention relates to a procedure for the production of tiacumicin B comprising fermentation of a micro-organism capable of producing tiacumicin B, in particular of the species Dactylosporangium aurantiacum or Actinoplanes deccanensis, in a culture broth containing emulsifiers, such as ethoxylated castor oil, in combination with antifoaming products and vegetable oils.
Abstract: The present invention relates to a process for obtaining Tiacumicin B with a well defined crystal habit and particle size. The process according to the invention comprises repeating cycles of heating and cooling under controlled conditions of temperature and stirring.
Abstract: Subject-matter of the invention is a process for the preparation of a key intermediate in the synthesis of indacaterol. Subject-matter of the invention are also new synthesis intermediates.
Abstract: Disclosed is a novel process for the synthesis of tofacitinib citrate on an industrial scale with high yields and purity starting with cis-(1-benzyl-4-methyl-piperidin-3-yl)methylamine bis-hydrochloride racemate (intermediate VIII), which comprises: 1. Condensation between intermediates VII and VIII to give intermediate VI 2. Hydrogenation of intermediate VI to give intermediate V 3. Resolution of intermediate V to give intermediate IV with enantiomeric purity >99% 4. Release of intermediate IV in a basic medium to give intermediate III 5. N-acylation reaction of intermediate III to give II (tofacitinib) 6.
Type:
Grant
Filed:
April 7, 2016
Date of Patent:
November 28, 2017
Assignee:
OLON S.P.A.
Inventors:
Jacopo Bonanomi, Stella Defiore, Barbara Novo
Abstract: The present invention refers to a new process for preparing levomilnacipran, in particular to a process for the resolution of racemic tw-milnacipran with a derivative of optically active phenylglycine.
Type:
Grant
Filed:
November 27, 2014
Date of Patent:
November 28, 2017
Assignee:
OLON S.P.A.
Inventors:
Paolo Maria Farina, René Ignacio Rodriguez Curiel, Stefano Maiorana, Aldo Bianchi, Federica Colombo, Gabriele Timpano
Abstract: The present invention concerns a new composition based on pellets of lipoic acid in a lipophilic medium, if necessary combined with other active ingredients.
Type:
Grant
Filed:
October 23, 2008
Date of Patent:
November 21, 2017
Assignee:
Olon S.p.A.
Inventors:
Paolo Magri', Antonio Nardi, Annibale Salvi, Flavio Villani
Abstract: The present invention refers to a process for the preparation of 1-(2-halogen-ethyl)-4-piperidinecarboxylic acid ethyl esters, in particular of 1-(2-chloroethyl)-4 piperidinecarboxylic acid ethyl ester, a versatile synthesis intermediate, particularly useful as an intermediate compound in the synthesis of umeclidinium.
Abstract: Disclosed is a process for the preparation of abiraterone and abiraterone acetate with high yields and purity. A key element of the method is the isolation of a crystalline intermediate that makes the process particularly suitable for implementation on an industrial scale.
Abstract: Disclosed is a process for the preparation of abiraterone and abiraterone acetate with high yields and purity. A key element of the method is the isolation of a crystalline intermediate that makes the process particularly suitable for implementation on an industrial scale. There is also provided a process for the production of abiraterone acetate by acetylation of abiraterone in the absence of bases or acetylation catalysts.
Abstract: Disclosed is asenapine phosphate of formula (I) and its enantiomer (I) which can be used to prepare asenapine maleate. Further disclosed is a monoclinic crystalline form of asenapine maleate.
Type:
Grant
Filed:
April 30, 2012
Date of Patent:
September 20, 2016
Assignee:
OLON S.P.A.
Inventors:
Samuele Frigoli, Davide Longoni, Tamara Danelli, Marco Alpegiani
Abstract: The invention relates to a process for the purification of crude abiraterone acetate by treatment with polymer resins in aqueous solvent. The purified product is recovered by simple concentration and filtration.
Type:
Grant
Filed:
October 21, 2013
Date of Patent:
May 17, 2016
Assignee:
OLON S.P.A.
Inventors:
Marco Alpegiani, Tania Cristiano, Eugenio Cucchetti
Abstract: Disclosed is a method for the conversion of a compound of formula 3 to a compound of formula 4, wherein R is an acetyl group or an alcohol-protecting group. The process involves reacting 3 with a triflating agent in the presence of a nicotinate (3-pyridinecarboxylate) of a C1-C4 alcohol, preferably methyl nicotinate (methyl 3-pyridinecarboxylate) or ethyl nicotinate (ethyl 3-pyridinecarboxylate), to give 4. The method can be conveniently used in a process for the preparation of Abiraterone or Abiraterone acetate.