17083-26-0Relevant articles and documents
Preparation method of fmoc-O-tert-butyl-L-serine
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Paragraph 0005; 0024; 0025; 0027; 0031; 0033; 0036; 0038, (2019/02/17)
The invention discloses a preparation method of fmoc-O-tert-butyl-L-serine. The method comprises the steps that 1, L-serine and a methanol solution are added into a reaction container, and under stirring, SOCl2 is added dropwise for reflux reaction to obtain L-serine methyl ester hydrochloride; 2, the L-serine methyl ester hydrochloride is added into tert-butyl acetate, and a catalyst is added forreaction to obtain O-tert-butyl-L-serine methyl ester; 3, the O-tert-butyl-L-serine methyl ester is added into alkaline liquid for saponification reaction to obtain an O-tert-butyl-L-serine aqueous solution; 4, an organic solvent and NaCO3 are added into O-tert-butyl-L-serine, then fmoc n-hydroxysuccinimide este is added to adjust a pH value to be 8-10, and extraction separation is conducted to obtain the fmoc-O-tert-butyl-L-serine. In the preparation method, the L-serine, methanol and SOCl2 are adopted as raw materials, and through the reflux reaction, the L-serine methyl ester hydrochlorideis prepared; the reaction is carried out in liquid phases respectively, and is safe and pollution-free.
Anthranilimide-based glycogen phosphorylase inhibitors for the treatment of Type 2 diabetes: 2. Optimization of serine and threonine ether amino acid residues
Sparks, Steven M.,Banker, Pierette,Bickett, David M.,Clancy, Daphne C.,Dickerson, Scott H.,Garrido, Dulce M.,Golden, Pamela L.,Peat, Andrew J.,Sheckler, Lauren R.,Tavares, Francis X.,Thomson, Stephen A.,Weiel, James E.
scheme or table, p. 981 - 985 (2009/08/15)
Optimization of the amino acid residue of a series of anthranilimide-based glycogen phosphorylase inhibitors is described leading to the identification of serine and threonine ether analogs. t-Butylthreonine analog 20 displayed potent in vitro inhibition of GPa, low potential for P450 inhibition, and excellent pharmacokinetic properties.
Novel conformationally constrained analogues of diacylglycerol. Protein kinase C binding affinity of simplified compounds based on a 6-membered lactam moiety
Endo, Yasuyuki,Hirano, Masaaki,Driedger, Paul E.,Stabel, Silvia,Shudo, Koichi
, p. 2997 - 3000 (2007/10/03)
Four configurational isomers of 6-hydroxymethyl-3-isopropyl-4-tetradecylpiperazin-2-ones (4-7), which were designed based on information obtained from the biologically active conformation of teleocidins and benzolactams, were synthesized and evaluated for