24630-68-0Relevant articles and documents
Chemoenzymatic Synthesis of Racemic and Enantiomerically Pure Phosphaaspartic Acid and Phosphaarginine
Qian, Renzhe,Kuliszewska, Edyta,Macoratti, Elena,Hammerschmidt, Friedrich
, p. 4836 - 4845 (2017)
Diisopropyl allyloxymethylphosphonate prepared by a one-pot procedure was isomerized to give racemic 1-hydroxy-3-butenylphosphonate with LDA by a [2,3]-sigmatropic rearrangement. Chloroacetylation delivered an ester, which was resolved in a two-phase system by using the lipase from Thermomyces lanuginosus. Racemic and (S)-α-hydroxyphosphonate 6 were converted to (±)- and (R)-phosphaaspartic acid by functional-group manipulation. (±)-, (R)- and (S)-6 were first esterified with 4-nitrobenzenesulfonyl chloride before hydroboration to transform the double bond into a hydroxyethyl group. The hydroxyl group was manipulated to give a guanidinyl group and the 4-nitrobenzenesulfonyloxy to give an amino group. Global deprotection of the α-aminophosphonates yielded the desired phosphaamino acids.
THYROID HORMONE RECEPTOR AGONIST AND USE THEREOF
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Paragraph 0128; 0129, (2017/11/15)
A thyroid hormone receptor agonist and its use in the treatment of a disease associated thyroid hormone receptor beta are described. The compound can be effective in lowering cholesterol with minimum or no adverse effects on the heart or thyroid hormone axis.
Copper-catalyzed synthesis of α-hydroxy phosphonates from H-phosphonates and alcohols or ethers
Zhao, Zengxiang,Xue, Wanhua,Gao, Yuxing,Tang, Guo,Zhao, Yufen
supporting information, p. 713 - 716 (2013/05/09)
Easy PC: α-Hydroxy phosphonates were synthesized by copper/tert-butyl hydroperoxide (TBHP)-catalyzed oxidative addition reactions of H-phosphonates with alcohols or ethers. Diverse α-hydroxy phosphonates were obtained from substituted benzyl alcohols or alkyl alcohols and alkyl ethers in moderate to good yields. Copyright