With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.31166-44-6,1-Cbz-Piperazine,as a common compound, the synthetic route is as follows.
Step A: Preparation of 2a; According to general procedure C, 2a was obtained with 1a (0.25 mL, 5.18 mmol, 1.0 eq.), EDC (324 mg, 10.36 mmol, 2.0 eq.), DMAP (317 mg, 10.36 mmol, 2.0 eq.) and N-methylpyrrole-2-carboxylic acid (329 mg, 10.36 mmol, 2.0 eq.). The mixture was washed first with a saturated solution of ammonium chloride, then with 1 N HCl and at the end with a saturated solution of sodium carbonate. The residue was purified by flash chromatography on silica gel, eluting with cyclohexane-ethyl acetate (8:2 to 1:1) to afford 2a (420 mg, 98percent) as a colorless oil.MS (ESI+) (+0.1percent HCOOH): 328.12 [C18H21N3O3+H]+ (m/z); “General method C” (peptide coupling) consists of adding 1.2 to 2.0 equivalents of EDCl and 1.2 to 2.0 equivalents of HOBt or DMAP and 1.2 to 2.0 equivalents of heteroaryl carboxylic acid, at 0¡ã C., to a 0.2 to 0.6M solution within DMF of protected amino(piperidine) derivative N-Boc or N-CBz. The mixture is maintained under stirring at ambient temperature for 16 to 18 hours, then diluted with ethyl acetate and washed with water. The solution is then dried and concentrated to dryness under reduced pressure, then the residue is purified by chromatography over silica eluting with the cyclohexane-ethyl acetate mixture., 31166-44-6
31166-44-6 1-Cbz-Piperazine 643495, apiperazines compound, is more and more widely used in various fields.
Reference£º
Patent; Vetoquinol SA; US2010/9980; (2010); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics