Downstream synthetic route of 1,4-Di-Boc-piperazine-2-carboxylic acid

181955-79-3, 181955-79-3 1,4-Di-Boc-piperazine-2-carboxylic acid 11255979, apiperazines compound, is more and more widely used in various fields.

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.181955-79-3,1,4-Di-Boc-piperazine-2-carboxylic acid,as a common compound, the synthetic route is as follows.

N,N-di-tert.butoxycarbonyl-3-carboxypiperazine (2gm, 6.2mm) was dissolved in 20 ml of N,N-dimethylformamide. 4-Pyrollidinoneaminopropane ( 12.4ml, 12.4mm), 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride (DEC) (2.38gm, 12.4mm), 1-hydroxybenzotriazole (HOBt) (1.68gm, 12.4mm), and N-methylmorpholine ( 6.82ml, 62mm) were added and the reaction mixture stirred at ambient temperature under a dry nitrogen atmosphere for 18 hours. The reaction mixture was added to brine and the product extracted with 3X159 ml of ethylacetate. The ethylacetate layers were dried over magnesium sulfate and evaporated under vacuo. The crude product was chromatographed on a silica gel column using 5% methanol/methylenechloride as the eluent to obtain the title product which was treated with 30 ml of trifluoroacetic acid for 4 hr at ambient temperature. The trifluoroacetic acid was evaporated to obtain 6 gm of a light brown oil.

181955-79-3, 181955-79-3 1,4-Di-Boc-piperazine-2-carboxylic acid 11255979, apiperazines compound, is more and more widely used in various fields.

Reference:
Patent; SCHERING CORPORATION; PHARMACOPEIA, INC.; EP989983; (2004); B1;,
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