298693-95-5Relevant academic research and scientific papers
Development of a scalable synthetic route towards a thrombin inhibitor, LB30057
Kim, Bong Chan,Hwang, Sang Yeul,Lee, Tae Hee,Chang, Jay Hyok,Choi, Hyeong-Wook,Lee, Kyu Woong,Choi, Bo Seung,Kim, Young Keun,Lee, Jae Hoon,Kim, Won Sup,Oh, Yeong Soo,Lee, Hee Bong,Kim, Kyu Young,Shin, Hyunik
, p. 881 - 886 (2012/12/23)
Described is a scalable synthetic route towards LB30057 (1) which is based upon a chiron approach using methyl tyrosinate hydrochloride as a starting material. In situ protection of methyl tyrosinate to its N,O-bis-trimethylsilyl derivative and subsequent N-selective introduction of naphthalenesulfonyl group provided methyl N-2-naphthalenesulfonyltyrosinate (9). After the phenol group of 9 was Inflated to 10, nickel-catalyzed cyanation provided 11 in good yield. The acid chloride 11a was generated via hydrolysis of the ester group followed by the treatment with SOCl2, and then coupled with cyclopentylmethylamine to give the amide 15. Imidate formation followed by amidrazone generation and final salt formation with maleic acid afforded 1.
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
Process for synthesizing para-and/or meta-substituted cyanophenylalanine 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 tha
