With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.137076-54-1,2-(4,7,10-Tris(2-(tert-butoxy)-2-oxoethyl)-1,4,7,10-tetraazacyclododecan-1-yl)acetic acid,as a common compound, the synthetic route is as follows.
A solution of the product of Example 3OB (30.0 mg, 63.8 mumol) and /-Pr2NEt (11 muL, 63 mumol) in dry DMF (1.00 mL) was transferred to a previously prepared solution of (4,7, 10-tris-f¡ãrt-butoxycarbonylmethyl- 1 ,4,7, 10-tetraazacyclododec- 1 – yl)acetic acid (47.5 mg, 82.9 mumol) in DMF (3.00 mL) containing HBTU (26.6 mg, 70.1 mumol), HOBt (10.7 mg, 69.9 mumol) and /-Pr2NEt (44 muL, 0.25 mmol); additional DMF (2 x 0.50 mL) was used to quantitate the transfer. The resulting solution was maintained at 22 C for 3 hours, then concentrated in vacuo and the residue treated with a solution OfEt3SiH in TFA (9:1 v/v, 3.30 mL). After stirring 2.5 hours at 22 0C, the resulting solution was concentrated in vacuo and purified by HPLC on a Phenomenex Luna C18 column (21.2 x 250 mm) using a 0.67%/min gradient of 0- 20% acetonitrile containing 0.1% TFA at a flow rate of 20 rnL/min. The main product peak eluting at 5.5 minutes was lyophilized to a white solid (65.0 mg, 53.6 mumol; 84.0%). MS (ESI): 643.3 (65.2, M+H), 530.3 (36.0), 322.3 (100, M+2H), 265.7 (49.7). HRMS: Calcd for C28H51N8O9: 643.3774; found: 643.3763. The optical purity of the product was established by chiral GLC analysis; 99.8% D- leucine.
137076-54-1, The synthetic route of 137076-54-1 has been constantly updated, and we look forward to future research findings.
Reference£º
Patent; BRISTOL-MYERS SQUIBB PHARMA COMPANY; WO2007/5491; (2007); A1;,
Metal catalyst and ligand design
Ligand Template Strategies for Catalyst Encapsulation – NCBI