The preparation of ester heterocycles mostly uses heteroatoms as nucleophilic sites, which are achieved by intramolecular substitution or addition reactions. Compound: (S)-4-((Benzyloxy)carbonyl)-1-(tert-butoxycarbonyl)piperazine-2-carboxylic acid( cas:138775-03-8 ) is researched.Formula: C18H24N2O6.Ibrahim, Mohamed A.; Johnson, Henry W. B.; Jeong, Joon Won; Lewis, Gary L.; Shi, Xian; Noguchi, Robin T.; Williams, Matthew; Leahy, James W.; Nuss, John M.; Woolfrey, John; Banica, Monica; Bentzien, Frauke; Chou, Yu-Chien; Gibson, Anna; Heald, Nathan; Lamb, Peter; Mattheakis, Larry; Matthews, David; Shipway, Aaron; Wu, Xiang; Zhang, WenTao; Zhou, Sihong; Shankar, Geetha published the article 《Discovery of a novel class of potent and orally bioavailable sphingosine 1-phosphate receptor 1 antagonists》 about this compound( cas:138775-03-8 ) in Journal of Medicinal Chemistry. Keywords: amide preparation sphingosine phosphate receptor antagonistic pharmacokinetics. Let’s learn more about this compound (cas:138775-03-8).
A series of subtype selective sphingosine 1-phosphate receptor 1 (S1P1) antagonists are disclosed. Our high-throughput screening campaign revealed hit I for which an increase in potency and mouse oral exposure was achieved with minor modifications to the chem. scaffold. In vivo efficacy revealed that at high doses compounds II(X = F, Cl) inhibited tumor growth. Further optimization of our lead series led to the discovery of proline derivatives III(R = 1,2,3-triazol-1yl) (XL541) and III(R = 1,2,3-triazol-2yl) which had similar efficacy as our first generation analogs at significantly lower doses. Analog III(R = 1,2,3-triazol-1yl) displayed excellent pharmacokinetics and oral exposure in multiple species.
After consulting a lot of data, we found that this compound(138775-03-8)Formula: C18H24N2O6 can be used in many types of reactions. And in most cases, this compound has more advantages.
Reference:
Iodide – Wikipedia,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com