Indena S.p.a.

Andrea Gambini

Pietro Allegrini

Daniele Ciceri

Bruno Gabetta

Nicola Sardone

Federico Peterlongo

Ezio Bombardelli

Walter Cabri

Gabriele Fontana

Maurizio Ricotti

Andrea Bonetti

Marco Molinari

Davide Berlanda

Fabio Donzelli

Stefano Luca Giaffreda

Luca Domenighini

Enrico Modena

Alessandro Andreani

Alex Petrolati

The invention relates to a process for the preparation of colchicine 1 from colchicoside 2 which comprises enzymatic conversion of colchicoside 2 to 3-O-demethylcolchicine 3, wherein the enzyme used is a cellulase. According to another aspect of the invention, 3-O-demethylcolchicine 3 can be converted to colchicine 1 using an alkylating agent. The invention also relates to a process for enriching the colchicine 1 content of extracts from plants belonging to the Colchicaceae family containing colchicine 1, colchicoside 2 and 3-O-demethylcolchicine 3, which comprises conversion by means of a colchicoside 2 cellulase to 3-O-demethylcolchicine 3, followed by conversion of 3-O-demethylcolchicine 3 to colchicine 1 using an alkylating agent.

Semisynthetic process for the preparation of colchicine

The invention relates to a process for the preparation of Melphalan (4-[bis(2-chloroethyl)amino]-L-phenylalanine of formula (I) The invention also provides novel intermediates useful for the preparation of Melphalan.

Process for the synthesis of melphalan

The invention relates to a process for the preparation of Melphalan (4-[bis(2-5 chloroethyl)amino]-L-phenylalanine of formula (I) said process comprising the reaction of a 4-amino-L-phenylalanine protected at the carboxy and amino aminoacidic groups with an agent able to convert the aromatic amino group into a group of formula: &#x2014;N(CHCHOS(O)O&#x2014;), wherein n is 1 or 2 followed by conversion of the &#x2192;N(CHCHOS(O)O&#x2014;)group into a &#x2014;N(CHCHCl)group. The invention also provides novel intermediates useful for the preparation of Melphalan.

Process for the synthesis of Melphalan

The present invention provides novel crystalline forms of 4-[3-Chloro-4-(N'-cyclopropylureido)phenoxy]-7-methoxyquinoline-6-carboxamide methanesulfonate, as well as methods for their preparation.

Crystal forms of lenvatinib

Disclosed are solid forms of ingenol 3-(3,5-diethylisoxazole-4-carboxylate) selected from an amorphous form or a crystalline anhydrous form. Also disclosed are solid solvates of ingenol 3-(3,5-diethylisoxazole-4-carboxylate) selected from an acetone solvate, a dimethylcarbonate solvate, an isopropyl ether solvate, an acetonitrile solvate, a toluene solvate, a mesitylene solvate, a nitromethane solvate, a dichloromethane/heptane solvate and an ethyl acetate solvate, for use as intermediates.

Solid forms of ingenol 3-(3,5-diethylisoxazole-4-carboxylate) and method for preparing the same

The present invention refers to an amorphous form of a thiocolchicine derivative, IDN 5404, to a process for producing it and to pharmaceutical compositions thereof. The amorphous form is characterized by the XRPD pattern, DSC profile and/or TG/DTA profile.

Amorphous form of a thiocolchicine derivative

The present invention relates to a new anhydrous crystalline form of Cabazitaxel of formula (I), designated as form H. A further object of the present invention is a processes for the preparation of the above mentioned form H by recrystallization of Cabazitaxel from a mixture of decanoyl- and octanoyl triglycerides or from glycerol trioctanoate. Form H of Cabazitaxel is useful for the preparation of Cabazitaxel, Cabazitaxel salts, and polymorphic forms thereof. It is also particularly useful as a medicament, especially for the treatment of cancers. 

Crystalline anhydrous form of Cabazitaxel, process for the preparation and pharmaceutical compositions thereof

A process for the preparation of 10-deacetyl-7,10-bis-trichloroacetylbaccatine III with HPLC purity higher than 99% and free from 2-debenzoyl-2-pentenoylbaccatine III by purification of 10-deacetyl-7,10-bis-trichloroacetylbaccatineIII followed by alkaline hydrolysis of the protecting groups in position 7 and 10.

Process for the purification 10-deacetylbaccatine III from 10-deacetyl-2-debenzoyl-2-pentenoylbaccatine III

A crystalline from of 13-[(N-tert-butoxycarbonyl)-2'-O-hexanoyl-3-phenylisoserinyl]-10-deacetylbaccatin III.

Crytalline form of 13-[(N-tert-butoxycarbonyl)-2'-O-hexanoyl-3-phenylisoserinyl]-10-deacetylbaccatin III

A process for the preparation of 10-deacetyl-bis-7,10-trichloroacetylbaccatin III (VI) 

Semisynthesis process for the preparation of 10 deacetyl-N-debenzoyl-paclitaxel

A process is provided for the preparation of 10-deacetyl-N-debenzoyl-paclitaxel (I) a synthon useful for the preparation of taxanes with antitumour activity, and intermediates for the preparation thereof. Also described is a process for the preparation of Docetaxel starting from the compound of formula (I).

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Milan, Italy

Andrea Gambini