1620097-07-5

Usage

Uses

Used in Pharmaceutical Industry:
Suvorexant intermediate is used as a key intermediate in the synthesis of Suvorexant for the treatment of insomnia. It is essential for the production of the final pharmaceutical drug, ensuring the effectiveness and safety of the medication.
Used in Insomnia Treatment:
Suvorexant intermediate is used as a precursor in the manufacturing of Suvorexant, which is a medication specifically designed to treat insomnia. It helps in the regulation of sleep-wake cycles, providing relief to individuals suffering from sleep disorders.

Upstream product

• 53386-64-4 methyl 2-(benzylamino)acetate 
• 956317-36-5 2-(2H-1,2,3-triazol-2-yl)-5-methylbenzoic acid 
• 1620097-06-4 (R)-1-benzyl-5-methyl-1,4-diazepane 
• 170367-70-1 [1(R)-methyl-3-[(phenylmethyl)amino]propyl]carbamic acid, 1,1-dimethylethyl ester 
• 1104546-96-4 5-methyl-2-(2Η-1,2,3-triazol-2-yl)benzoyl chloride 

Downstream Products

• 1030377-32-2 1-(7(R)-methyl-1,4-diazepan-1-yl)-1-[5-methyl-2-(2H-1,2,3-triazole-2-yl)phenyl]methanone 
• 1030377-33-3 Suvorexant 

Relevant academic research and scientific papers

Preparation method of raw drug suvorexant

The invention discloses a preparation method of raw drug suvorexant. The preparation method comprises the following step of generating S1 condensation acylation reaction by virtue of an intermediate I and an intermediate II in the presence of a condensing agent so as to generate an intermediate III, wherein the condensing agent is selected from one or combination of more than two of ethyl-(3-dimethylaminopropyl)carbodiimide hydrochloride, N,N'-carbonyldiimidazole, 1-hydroxybenzotriazole, 1-hydroxy-7-azobenzotriazole and tri(2,6-dimethoxyphenyl)bismuth. By adopting the proper condensing agent or condensing agent combination in the S1 condensation acylation reaction in the preparation method, and the yield in the prior art can be achieved at a reaction temperature of about 25 DEG C, and the condensing agent and intermediate products are simply separated, so that the energy saving and the consumption reduction in the large-scale industrial production are promoted.

Used for preparing suvorexant compound and method for preparing same

The invention relates to three novel compound formulas I, II and III for preparing suvorexant, stereoisomers or salt thereof and a preparation method of the formulas I, II and III. The invention also relates to a method for preparing the suvorexant. The preparation method disclosed by the invention can be used for synthesizing to obtain the chiral compounds I, II and III through a chiral initiator and use the chiral compounds I, II and III for the synthesis of the suvorexant and has the advantages of easiness for operation, moderation in reaction condition, easiness for post processing, easiness for purification, high yield, high ee value and easiness for industrialization.

Preparation method of chiral high piperazine ring compound

The present invention relates to a preparation method of a chiral high piperazine ring compound shown in (R)-I, and the method includes reduction of a compound shown in a formula Int to obtain the compound shown in the formula (R)-I. The invention also relates to a novel intermediate compound shown in the formula Int. The chiral high piperazine ring compound shown in (R)-I is an important intermediate in the synthesis of a medicament Suvorexant for the treatment of sleep disorders. The preparation method introduces a chiral center from the starting material, does not employ reagent or reaction affecting the chiral center in the whole reaction process, and avoids the chiral resolution or chiral catalyst method, which has high cost but low yield; no reaction of chiral participation exists in the process, so as to ensure the purity of the chiral product; and the method uses only the conventional methods and equipment, has the advantages of simple operation, mild condition, short route and high yield, and is applicable to industrialized production.

PROCESS FOR THE PREPARATION OF SUVOREXANT AND INTERMEDIATES USEFUL IN THE SYNTHESIS OF SUVOREXANT

A novel processes for the preparation of suvorexant (formula I), its related compounds and its intermediates that are simple, economical and commercially viable. (I)

Facile synthesis of suvorexant, an orexin receptor antagonist, via a chiral diazepane intermediate

A facile synthesis of suvorexant, an orexin receptor antagonist, is described. The key intermediate 6 was prepared from R-3-aminobutyric acid through protection, condensation, deprotection, cyclization, and hydrogenation steps. The title product was obtained with a total yield of 31% (>99% ee) after eight linear steps using commercially available raw materials.