163343-71-3Relevant articles and documents
Synthetic method for (R)-N-tert-butoxycarbonyl-3-hydroxymethylpiperidine
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, (2019/08/12)
The invention discloses a synthetic method for (R)-N-tert-butoxycarbonyl-3-hydroxymethylpiperidine. The method comprises the following four steps: synthesizing ethyl 3-piperidinecarboxylate (compoundII), synthesizing ethyl (R)-nipecotate-L-tartarate (compound III), synthesizing ethyl (R)-N-Boc-3-piperidinecarboxylate (compound IV) and synthesizing the (R)-N-tert-butoxycarbonyl-3-hydroxymethylpiperidine (compound V); and the method comprises the following special steps: synthesizing the compound II by using 3-piperidinecarboxylic acid (compound I) as a raw material through chloroacylation andethanol esterification; performing a salt formation reaction to form the compound III; adding a Boc anhydride and performing a reaction to obtain the compound IV; and finally performing sodium borohydride reduction to obtain the compound V. The method provided by the invention has the advantages of mild reaction conditions, environmental friendliness, simple operation steps, better reproducibilityand high practicability, and is suitable for industrial mass production of the (R)-N-tert-butoxycarbonyl-3-hydroxymethylpiperidine.
FARNESYL PROTEIN TRANSFERASE INHIBITORS
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Page/Page column 33, (2010/02/11)
Disclosed are compounds of formula (1.0), wherein R represents a cyclic moiety to which is bound an imodazolylalkyl group; R represents a carbamate, urea, amide or sulfonamide group; and the remaining substituents are as defined herein. Also disclosed is a method of treating cancer and a method of inhibiting farnesyl protein transferase using the disclosed compounds.
A Practical Synthesis of the Platelet Fibrinogen Antagonist, Elarofiban
Cohen, Judith H.,Roessler, Armin,Scott, Lorraine,Sorgi, Kirk L.,Villani Jr., Frank J.,Webster, Robin R. H.,Weh, Christian,Bos, Mary Ellen,Cesco-Cancian, Sergio,Harris, Bruce D.,Hortenstine, John T.,Justus, Michael,Maryanoff, Cynthia A.,Mills, John,Muller, Stefan
, p. 866 - 872 (2013/09/05)
Elarofiban is a novel, nonpeptide, orally active fibrinogen receptor antagonist useful for the treatment of platelet mediated thrombotic disorders (Costanzo, M. J.; Hoekstra, W. J.; Maryanoff, B. E. WO, 97/41102,1997). Herein we describe the process research that was carried out for the synthesis of elarofiban that eventually led to the development of a safe and cost-effective commercial scale process.