552292-08-7

Usage

Uses

Used in Pharmaceutical Industry:
Rolapitant is used as an antiemetic agent for the prevention of delayed nausea and vomiting associated with initial and repeat courses of emetogenic cancer chemotherapy. It works by blocking the neurokinin-1 (NK-1) receptor, which is involved in the vomiting reflex, thus providing relief to patients undergoing cancer treatment.

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Downstream Products

• 858102-80-4 (5S,8S)-8-[{(1R)-1-(3,5-bis-(trifluoromethyl)phenyl)-ethoxy}-methyl]-8-phenyl-1,7-diazaspiro[4.5]decan-2-one tosylate 
• 914462-92-3 (5S,8S)-8-[{(1R)-1-(3,5-bis-(trifluoromethyl)phenyl)-ethoxy}-methyl]-8-phenyl-1,7-diazaspiro[4.5]decan-2-one hydrochloride monohydrate 
• 951390-95-7 (5S,8S)-8-[{(1R)-1-(3,5-bis-(trifluoromethyl)phenyl)-ethoxy}-methyl]-8-phenyl-1,7-diazaspiro[4.5]decan-2-one esylate 
• 951390-96-8 (5S,8S)-8-[{(1R)-1-(3,5-bis-(trifluoromethyl)phenyl)-ethoxy}-methyl]-8-phenyl-1,7-diazaspiro[4.5]decan-2-one oxalate 
• 951390-97-9 (5S,8S)-8-[{(1R)-1-(3,5-bis-(trifluoromethyl)phenyl)-ethoxy}-methyl]-8-phenyl-1,7-diazaspiro[4.5]decan-2-one mesylate 
• 951390-98-0 (5S,8S)-8-[{(1R)-1-(3,5-bis-(trifluoromethyl)phenyl)-ethoxy}-methyl]-8-phenyl-1,7-diazaspiro[4.5]decan-2-one maleate 

Relevant academic research and scientific papers

A NK - 1 receptor antagonists of the preparation method and its intermediate

The invention relates to a preparation method of an NK-1 receptor antagonist and an intermediate thereof. The invention provides a preparation method of (5S, 8s)-8-{[1-(3, 5-bis-(trifluoromethyl)phenyl)-ethoxy]methyl}-8-phenyl-1, 7-diaza-spiro[4, 5]dec-2-one (formula I compound), which is prepared from a formula II compound, and also provides the formula II compound and a preparation method thereof. The method provided by the invention has the advantages of simple operation, mild reaction condition, high safety factor, little side reaction, high yield and high purity, lowers the production cost and operation risk, and is very suitable for large-scale industrial production. (formula II as shown in the specification).

Synthesis method of rolapitant

The invention provides a synthesis method of a compound rolapitant shown in a formula (1). The synthesis method comprises the following step: by taking a compound in a formula (2) as a starting raw material, performing a series of following reactions so as to finally obtain the compound, namely rolapitant in the formula (1). Compared with the situation in the prior art that the rolapitant synthesis steps are more and the synthesis technology is complicated, the synthesis method is simple and feasible, low in cost, high in yield, good in the quality of products, and suitable for large industrial production.

And as the antagonist aminopyrrolidine deriv. NK1 aminopiperidine (by machine translation)

A NK 1 antagonist having the formula (I), wherein Ar 1 and Ar 2 are optionally substituted phenyl or heteroaryl, X 1 is an ether, thio or imino linkage, R 4 and R 5 are not both H or alkyl, and the remaining variables are as defined in the specification, useful for treating a number of disorders, including emesis, depression, anxiety and cough. Pharmaceutical compositions. Methods of treatment and combinations with other agents are also disclosed.

PROCESS AND INTERMEDIATES FOR THE SYNTHESIS OF 8-[-METHYL]-8-PHENYL-1,7-DIAZA-SPIRO[4.5]DECAN-2-ONE COMPOUNDS

This application discloses a novel process to synthesize 8-[{1-(3,5-Bis-(trifluoromethyl)phenyl)-ethoxy}-methyl]-8-phenyl-1,7-diaza-spiro[4.5]decan-2-one compounds, which may be used, for example, as NK-1 inhibitor compounds in pharmaceutical preparations.

Hydrochloride salts of 8-[{1-(3,5-Bis-(trifluoromethyl)phenyl)-ethoxy)-methyl]-8-phenyl-1,7-diaza-spiro[4.5]decan-2-one and preparation process therefor

Disclosed are hydrochloride and tosylate crystalline salt forms of (5S,8S)-8-[{(1R)-1-(3,5-Bis-(trifluoromethyl)phenyl)-ethoxy}-methyl]-8-phenyl-1,7-diazaspiro[4.5]decan-2-one, represented by Formula I and methods of preparing the same.