With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.288851-44-5,4-(4-(tert-Butoxycarbonyl)piperazin-1-yl)-4-oxobutanoic acid,as a common compound, the synthetic route is as follows.
To a solution of Boc-piperazine (P/N: Lancaster L13363, 500 mg, 2.68 mmol) in DCM(30 ml) was added succinic anhydride (269 mg, 2.68 mmol). The reaction was stirred for 2 hours at ambient temperature. TLC analysis showed formation of succinylated Boc-piperazine (Rf= 0.50; 9:1:0.01 DCM-MeOH-AcOH, TLC developed by heating with 3% (w/v) solution of ninhydrin in EtOH). To this solution was added TFA (30 mL) and the mixture was then stirred for 1 h at ambient temperature. The volatile components of the mixture were removed under reduced pressure and the resulting oil dissolved in THF (30 mL) with minimum amount of water and adjustment of the pH to 9 by the addition of DIPEA. A solution of Fmoc-OSu (907 mg, 2.69 mmol) in THF (10 mL) was added and stirred for 1 h at ambient temperature. TLC analysis showed formation of a product (Rf = 0.55; 9:1:0.01 DCM-MeOH-AcOH, UV 254 nm, TLC developed by heating with 3% (w/v) solution of ninhydrin in EtOH). The volatile components of the mixture were then removed under reduced pressure and the resulting oil was dissolved in minimum volume of saturated NaHCO3. The aqueous solution was then extracted with Et2O (100 mL x 2), acidified (pH ~1) with HCI (1 M) and re-extracted with EtOAc (150 mL x 2). The combined EtOAc layers were dried over Na2SO4 and concentrated to give the product as colorless oil., 288851-44-5
The synthetic route of 288851-44-5 has been constantly updated, and we look forward to future research findings.
Reference£º
Patent; APPLERA CORPORATION; WO2007/87534; (2007); A2;,
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