89004-82-0Relevant articles and documents
BIARYL MONOBACTAM COMPOUNDS AND METHODS OF USE THEREOF FOR THE TREATMENT OF BACTERIAL INFECTIONS
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Page/Page column 230, (2017/07/06)
The present invention relates to biaryl monobactam compounds of Formula I: and pharmaceutically acceptable salts thereof, wherein X, Y, Z, A1, Q, A2, M, W, RX and Rz are as defined herein. The present invention also relates to compositions which comprise a biaryl monobactam compound of the invention or a pharmaceutically acceptable salt therof, and a pharmaceutically acceptable carrier. The invention further relates to methods for treating a bacterial infection comprising administering to the patient a therapeutically effective amount of a compound of the invention, either alone or in combination with a therapeutically effective amount of a second beta-lactam antibiotic.
SULFONYL AMIDE DERIVATIVES FOR THE TREATMENT OF ABNORMAL CELL GROWTH
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Page/Page column 40, (2009/04/24)
The present invention relates to a compound of the formula I wherein R1 to R6, A, B, n and m are as defined herein. Such novel sulfonyl amide derivatives are useful in the treatment of abnormal cell growth, such as cancer, in mammals. This invention also relates to a method of using such compounds in the treatment of abnormal cell growth in mammals, especially humans, and to pharmaceutical compositions containing such compounds.
Direct Synthesis of N-Protected Chiral Amino Acids from Imidodicarbonates employing either Mitsunobu or Triflate Alkylation. Feasibility Study using Lactate with Particular Reference to 15N-Labelling
Degerbeck, Fredrik,Fransson, Bengt,Grehn, Leif,Ragnarsson, Ulf
, p. 245 - 254 (2007/10/02)
Two novel approaches to N,N-diprotected chiral α-amino acid esters, based on selected imidodicarbonates as amine synthons, have been explored.Thus, N-alkylation of these substrates was smoothly accomplished by the Gabriel or Mitsunobu methods as well as by the use of triflates.Ethyl (R,S)-2-bromopropionate underwent nucleophilic substitution when treated with the potassium salt of selected imidodicarbonates in dry dimethylformamide to furnish the corresponding fully blocked (R,S)-alanines in high yield. the chirality of ethyl (S)-lactate was largely conserved when it was condensed with free imidodicarbonates and tosylcarbamates under conventional Mitsunobu conditions.The yield of the corresponding N,N-di-protected ethyl (R)-alaninate was strongly dependent of the electron-withdrawing properties of the imidodicarbonate alkyl groups.Thus, Boc2NH gave 5 percent of the product whereas Troc-NH-Z afforded the corresponding analogue in 83 percent yield under comparable conditions.On the other hand, triflates of various lactic acid esters reacted smoothly with the lithium salt of Boc2NH, also with clean inversion, as a result of which, after selective removal of two blocking groups, the N-protected alanine of opposite configuration could be isolated in high yield and excellent stereochemical purity.Both methods have been used for the synthesis of 15N-labelled N-protected (R)- and (S)-alanines, suitable for direct application to peptide synthesis.