Preparation of Intermediates for Organic Synthsis
Article Sidebar
Main Article Content
Abstract
Several synthetic methods are described for the preparation of compounds such as derivatives of natural amino acids, unnatural amino acids, amino esters, oxime esters and amino amides that may serve as intermediates in the synthesis of active pharmaceutical ingredients (APIs) or drugs. The compounds described herein are produced in high yield and purity and the synthetic procedures are detailed along with the NMR spectra of the compounds and useful chemical data relating to these compounds.
Article Details
References
Tailor-made amino acids in the design of small-molecule blockbuster drugs, Jianlin Han, Hiroyuki Konno, Tatsunori Sato, Vadim A. Soloshonok and Kunisuke Izawa, European Journal of Medicinal Chemistry, Vol. 22, 2021, 113448.
Structural, metabolic and ionic requirements for the uptake of L-carnitine by primary rat cortical cells, M.A.Virmani, S.Rossi, R.Conti, A.Spadoni, E.Arrigoni-Martinelli and M.Calvani, Pharmacol. Res., Vol. 33, Issue 1, 19-27, (1996).
Biaryl substituted 4-aminobutyric acid amides, Gary Ksander, Ciba Geigy Corp., US patent 5,217,996.
Facile synthesis of thalidomide, Binh Duong Vu, Ngoc Minh Ho Ba and Dinh Chau Phan, Org. Process Res. Dev. 2019, 23, 7, 1374.
Benzyl mono-p-fluorophosphonate and benzyl penta-fluorophosphate anions are physiologically stable phosphotyrosine mimetics and inhibitors of protein tyrosine phosphatases, Stefan Wagner and Matteo Accorsi, Chemistry, a European Journal, 23(61), 15387-15395 (2017).
Process for the preparation of valsartan, Zvi Harel and Igor Rukhman, Teva Pharmaceutical Industries Ltd., US Patent 7,378,531.
Novel piracetam synthetic method, Wenrui Diao, Zhengxiang Jiang, Zhenfeng Song, Hexian Yu, Zihua Wang and Feng Zhang, Shanghai Modern Hasen Shangqui Pharmaceutical Co. Ltd., Patent application CN102718691.
Counteracting psychotic effects of cytostatic drugs - by administration of nootropic agent, especially piracetam, UCB SA, Patent BE892942.
Process for the preparation of levetiracetam, its intermediate and the use of levetiracetam in pharmaceutical compositions, Kumar Yatendra, Prasad Mohan, Sing Kaptan, Arora Surinder Kumar, Dhingra Surinder Kumar, Ranbaxy Lab. Ltd., Patent application WO2006/090265.
The preparation of hydroxypyrazines and derived chloropyrazines, George Karmas and Paul E. Spoerri, Journal of American Chemical Society, 1952, 74, 1580-1584.
On the preparation and properties of some amino acid amides, Robert Warner Chambers and Frederick H. Carpenter, Journal of American Chemical Society, 1955, 77, 1522-1526.
Renin inhibitors containing 5-amino-2,5-disubstituted-4-hydroxypentanoic acid residues, Edward F. Kleinman, Robert L. Rosati and Jasjit S. Bindra, Pfizer Inc. US patent 4,729,985.
Synthesis and Antifungal Activity of Novel 1,5-diphenyl-1,4-pentadien-3-one oxime esters LI Shao-Bo, HU De-Yu, SONG Bao-An, YANG Song, JIN Lin-Hong, XUE Wei, ZENG Song, WANG Jun, CHEN Zhuo, LU Ping, ZHOU Xia and FAN Ling-E, Chinese Journal of Organic Chemistry No. 2, Vol. 28, 311-316, 2008.