ChemicalBook CAS DataBase List Buspirone

Buspirone synthesis

10synthesis methods

Product Name:Buspirone
CAS Number:36505-84-7
Molecular formula:C21H31N5O2
Molecular Weight:385.5

Buspirone, 8-[4-[4-(2-pyrimidyl)-1-piperazinyl]butyl]-8-azaspiro [4,5] decan-7,9-dione (5.2.6), is synthesized by the reaction of 1-(2-pyrimidyl)-4- (4-aminobutyl)piperazine (5.2.4) with 8-oxaspiro[4,5]decan-7,9-dione (5.2.5). In turn, 1- (2-pyrimidyl)-4-(4-aminobutyl)piperazine (5.2.4) is synthesized by the reaction of 1-(2-pyrimidyl)piperazine with 4-chlorobutyronitrile, giving 4-(2-pyrimidyl)-1-(3- cyanopropyl)piperazine (5.2.3), which is hydrogenated with Raney nickel into buspirone (5.2.4) [51–55].

1722-12-9 Synthesis

1722-12-9
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8-Azaspiro[4.5]decane-7,9-dione, 8-[4-(1-piperazinyl)butyl]-

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36505-84-7
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Yield:36505-84-7 90%

Reaction Conditions:

with C₄₈H₅₅ClN₂Pd;sodium t-butanolate in 1,2-dimethoxyethane at 20; for 16 h;Inert atmosphere;Sealed tube;

Steps:

9.3 (3) Synthesis of Buspar
In a N2 environment, compound 1n (1.0mmol, 1.0equiv), compound 2n (1.2equiv), Pd-NHC-1 (5mol%), sodium tert-butoxide (1.2equiv), 4mL ethylene glycol dimethyl ether, The mouth of the bottle was sealed and stirred for 16 hours under nitrogen at room temperature. Dilute with water, extract 3 times with ethyl acetate, spin dry under reduced pressure, dry with anhydrous sodium sulfate, and obtain a white solid after silica gel column chromatography with a yield of 90% (346.8 mg).

References:

Sun Yat-sen University;Qiu Liqin;Ouyang Jiasheng CN112209972, 2021, a Location in patent:Paragraph 0195; 0202-0204

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