- IMPROVED PROCESS FOR PREPARING OZANIMOD
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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.
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- Preparation method of ozanimod and intermediate thereof
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The invention relates to a preparation method of ozanimod and an intermediate thereof, and belongs to the field of medicinal chemistry. The preparation method comprises the following steps: oxidizinga sulfonamide substrate to obtain a sulfamide compound, and carrying out substitution and other reactions to obtain ozanimod. The method disclosed by the invention does not need to use a sodium-hydrogen reagent with high risk, has the advantages of high yield, high purity of the obtained ozanimod intermediate, convenience in operation and good safety, and is suitable for industrial amplification.
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- PROCESS FOR THE PREPARATION OF SPHINGOSINE-1-PHOSPHATE RECEPTOR AGONIST
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Industrially viable and advantageous processes for the preparation of Ozanimod are described. The invention also discloses the intermediates obtained in the process.
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- IMPROVED PROCESS FOR THE PREPARATION OF OZANIMOD Α-AMINO COMPOUND
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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.
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Page/Page column 23-24
(2019/04/16)
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- COMPOUNDS AND METHODS FOR TREATING LUPUS
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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
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Page/Page column 70; 71; 72; 73
(2018/04/17)
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- PROCESS FOR THE PRODUCTION OF OZANIMOD
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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.
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Page/Page column 30
(2018/12/13)
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- Preparation method for ozanimod and intermediate thereof
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The invention provides a preparation method for ozanimod and an intermediate thereof. The preparation method comprises the following steps: taking 2,3-dihydro-4-cyano-1-indanone as a raw material, andpreparing a compound III through a proper method; adopting a protecting agent to protect amido and hydroxyl of the compound III, thereby preparing a compound IV; performing salt treatment on the compound IV to prepare a compound V; performing ring-closure reaction on the compound V and a compound VI to prepare a compound VII; and performing deprotection on the compound VII to prepare ozanimod. Compared with the conventional method, the preparation method reduces reaction steps, increases the total yield, and the prepared products are high in quality; and the reaction conditions are gentle, dangerous operation conditions are avoided, application of highly toxic reagents and expensive chemical reagents is avoided, the safety problem in the conventional method is solved, and the cost is reduced, and the preparation method is suitable for industrial production.
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Paragraph 0090-0092
(2018/11/22)
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- A [...] and intermediate preparation method (by machine translation)
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The present invention provides [...] and intermediate preparation method. The method of the invention is to 2, 3 - dihydro - 4 - cyano - 1 - indenone as raw materials, through a suitable process for making the compound III. The protective agent to the compound III and protect hydroxy amino, compound IV is prepared. The compound IV is carried out to obtain compound V salt treatment. The compound V with compound VI to cyclization reaction to obtain compound VII. To the compound VII is prepared to carry out the deprotection [...]. The method of the invention compared with the traditional method, thereby reducing the reaction steps, improving the overall yield, preparing the product quality is high; mild reaction conditions, to avoid dangerous operating conditions, highly toxic reagent and expensive application of the chemical reagent, in the traditional method not only solves the safety problem, but also reduces the cost, and is suitable for industrial production. (by machine translation)
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Paragraph 0087; 0088; 0089
(2018/11/22)
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