183021-88-7Relevant articles and documents
METHODS AND SYSTEMS FOR PREPARING IRREVERSIBLE INHIBITORS OF PROTEIN TYROSINE PHOSPHATASES
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Page/Page column 20, (2011/10/03)
Described herein are the preparation and use of novel bromo- phosphonomethylphenylalanine amino acid derivatives (BrPmp) and BrPmp-containing peptides as specific, irreversible protein tyrosine phosphatase inhibitors, which are suitable for application in peptide synthesis. These derivatives are particularly advantageous since their synthesis is both easy and scalable, and they are suitable for peptide synthesis. The BrPmp derivatives described herein can be appropriately protected to allow for solid phase peptide synthesis (SPPS) and incorporation into peptides for preparation of protein tyrosine phosphatase inhibitors and inhibitor libraries. The peptides and peptide libraries can be used to identify new protein tyrosine phosphatase specific sequences and profile protein tyrosine phosphatase activity in cell lysates, diagnostic samples and biopsy samples.
Process for synthesizing para-and/or meta-substituted cyanophenyalanine derivatives
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, (2008/06/13)
The present invention relates to a process for preparing a useful medicinal intermediate represented by the following formula (1): in which, R1, A and n are defined as described in the specification, or its stereoisomer, characterized in that a
Stereocontrolled synthesis of hydroxymethylene phosphonate analogues of phosphorylated tyrosine and their conversion to monofluoromethylene phosphonate analogues
Yokomatsu, Tsutomu,Yamagishi, Takehiro,Matsumoto, Keita,Shibuya, Shiroshi
, p. 11725 - 11738 (2007/10/03)
A stereocontrolled synthesis of protected variants 13 and 15 of HPmp 2, a mimic of phosphorylated tyrosine, was achieved through either chiral-auxiliary assisted or chiral heterobimetal catalyzed stereoselective hydrophosphonylation of 4-formyl-L-phenylalanine derivative 7. Fluorination of HPmp derivatives 13 and 15 thus obtained was carried out to give FPmp derivatives 16 and 17.
