1306760-86-0Relevant academic research and scientific papers
Enantioselective Synthesis of Ozanimod, the Active Pharmaceutical Ingredient of a New Drug for Multiple Sclerosis
Cianferotti, Claudio,Barreca, Giuseppe,Bollabathini, Venkatesh,Carcone, Luca,Grainger, Damian,Staniland, Samantha,Taddei, Maurizio
, p. 1924 - 1930 (2021/04/05)
We report here a short enantioselective synthesis of Ozanimod, a potent modulator of the enzyme Sphingosine-1-phosphate receptor (S1PR), recently approved by FDA and EMA for the treatment of relapsing-remitting multiple sclerosis. Amongst different synthetic approaches explored, we achieved the best result introducing the stereogenic centre in the last step through imine asymmetric transfer hydrogenation (ATH) using Wills’ catalysts. Besides the reduced numbers of enantiomeric purity controls required, this process culminates in an exceptionally high enantioselective reductive amination obtained with commercially available tethered Ru catalysts. Starting from commercially available 4-cyano-indanone, enantiomerically pure Ozanimod was obtained in 5 steps in 62 % overall yield and 99 % ee.
IMPROVED PROCESS FOR PREPARING OZANIMOD
-
Page/Page column 9-10, (2021/02/12)
The present invention relates to the process of preparation of compound of formula (I) or a salt thereof. Further it relates to the solid form of compound (I).
IMPROVED PROCESS FOR PREPARING OZANIMOD
-
, (2020/07/04)
The presented invention relates to a process for preparation of compound of formula (1) or a salt thereof (i.e.) ozanimod : (1). The invention also relates to intermediates used in the process.
PROCESS FOR THE PREPARATION OF SPHINGOSINE-1-PHOSPHATE RECEPTOR AGONIST
-
Page/Page column 61-63, (2020/05/13)
Industrially viable and advantageous processes for the preparation of Ozanimod are described. The invention also discloses the intermediates obtained in the process.
A PROCESS FOR THE PREPARATION OF OZANIMOD AND ITS INTERMEDIATE (S)-1-AMINO-2,3-DIHYDRO-1H-INDENE-4-CARBONITRILE
-
Page/Page column 18-20, (2020/05/07)
The present invention relates to an improved process for preparation of Ozanimod (I) or pharmaceutically acceptable salts thereof. The present invention also relates to an improved process for preparation of (S)-l-amino-2,3-dihydro- 1H-indene-4-carbonitrile (II) or its optically active acid salts.
IMPROVED PROCESS FOR THE PREPARATION OF OZANIMOD Α-AMINO COMPOUND
-
, (2019/04/16)
The present invention relates to an improved process for the preparation of optically chiral amino compound. The present invention particularly relates to the improved process for the preparation of (S)-1-amino-2,3-dihydro-1H-indene-4-carbonitrile, an important intermediate for the synthesis of ozanimod. The present invention more particularly relates to preparation of (S)-1-amino-2,3-dihydro-1H-indene-4- carbonitrile using 4-cyano-1-indanone and α-methylbenzylamine derivatives as starting materials. The present invention specifically relates to preparation of (S)-1- amino-2,3-dihydro-1H-indene-4-carbonitrile comprising diastereoselective chiral amine synthesis by protection with chiral auxiliary ?-methyl benzylamine derivatives followed by reduction and debenzylation.
SALTS AND SOLID STATE FORMS OF OZANIMOD
-
Paragraph 00115, (2019/05/30)
Disclosed are Ozanimod solid state forms, salts including hydrochloride and solid state thereof, processes for preparation thereof, pharmaceutical compositions thereof, and methods of use thereof.
CRYSTALLINE FORMS OF OZANIMOD AND OZANIMOD HYDROCHLORIDE, AND PROCESSES FOR PREPARATION THEREOF
-
Paragraph 0178; 0180, (2019/11/19)
The present disclosure is directed to novel crystalline forms of ozanimod and ozanimod hydrochloride, as well as preparation method thereof. Said crystalline forms of ozanimod and ozanimod hydrochloride can be used for treating autoimmune diseases, partic
PROCESS FOR THE PRODUCTION OF OZANIMOD
-
, (2018/12/13)
The present invetion relates a new process for the preparation of ozanimod of the formula and acid addition salts, via new intermediates and a new polimop form of ozanimod base.
COMPOUNDS AND METHODS FOR TREATING LUPUS
-
Page/Page column 70; 71; 72; 73, (2018/04/17)
Methods for treatment of systemic lupus erythematosus (SLE" or "Lupus") by administration of a modulator of sphingosine-1-phosphate receptor subtype 1 (S1P1), as well as compositions and methods related to the same, wherein such S1P1 modulators have the f
