专利号:US-2010184989-A1 优先权日:2007-03-12 标 题 :De Novo Synthesis of Conjugates 发明人:RIGGS-SAUTHIER JENNIFER; DENG BO-LIANG; REN ZHONGXU; ZHANG WEN; GU XUYUAN; DUARTE FRANCO J 权利人:NEKTAR THERAPEUTICS 摘要:The invention provides methods for the preparation of small molecule drugs that are chemically modified by covalent attachment of a water-soluble oligomer obtained from a water-soluble oligomer composition. Such drugs are produced through modification of a synthetic pathway to attach the oligomer to an intermediate compound followed by completion of the synthetic path.
专利号:US-6573388-B1 优先权日:1999-08-18 标 题:Ethylaziridine derivatives and their preparation methods 发明人:KIM BYUNG MOON; BAE SUNG JIN; SO SOON MOK; KANG JAE SUNG; LEE JOONG HWAN 权利人:SAMCHULLY PHARM CO LTD 摘要:This invention is related to new ethylaziridine derivatives of formula (I) and their preparation. The compounds are useful synthetic intermediates for the synthesis of HIV protease inhibitors and oligopeptide mimetics.
专利号:JP-2010521465-A 优先权日:2007-03-12 标 题 :De novo synthesis of complex
专利号:JP-2013253104-A 优先权日:2007-03-12 标题:De novo synthesis of complex
专利号:US-5550291-A 优先权日:1994-12-06 标 题:Process for key intermediates for HIV protease inhibitors 发明人:BEAULIEU PIERRE L; GUINDON YVAN; WERNIC DOMINIK M 权利人:BIO MEGA BOEHRINGER INGELHEIM 摘要:Disclosed herein is a stereospecific synthesis amenable to the large scale preparation of a hydrochloric acid addition salt of a chlorohydrin of the formula ##STR1## wherein R 1 and R 2 are amino protective groups and R 3 is an amino acid side chain or a protected amino acid side chain. The synthesis involves reacting an aldehyde of the formula ##STR2## wherein R 1 , R 2 and R 3 are as defined hereinbefore with (chloromethyl)lithium at -20° C. or below and contacting the resulting diastereoisomeric mixture of lithium alcoholates with aqueous hydrochloric acid to obtain a separable mixture of the hydrochloric acid addition salts of the chlorohydrin and its corresponding hydroxy diastereoisomer. The hydrochloric acid addition salt of the chlorohydrin is transformed readily into corresponding optionally amino-protected aminoepoxides; for example, 3(S)-(tert-butyloxycarbonylamino)-l,2(S)-epoxy-4-phenyl-butane.
[参考文献]: Akbar Ali, Et Al. Discovery Of Hiv-1 Protease Inhibitors With Picomolar Affinities Incorporating N-Aryl-Oxazolidinone-5-Carboxamides As Novel P2 Ligands. J Med Chem. 2006 Dec 14;49(25):7342-56. [参考文献]: Arun K Ghosh, Et Al. Structure-Based Design Of Novel Hiv-1 Protease Inhibitors To Combat Drug Resistance. J Med Chem. 2006 Aug 24;49(17):5252-61. [参考文献]: William P Esler, Et Al. Probing Pockets S2-S4' Of The Gamma-Secretase Active Site With (Hydroxyethyl)Urea Peptidomimetics. Bioorg Med Chem Lett. 2004 Apr 19;14(8):1935-8.
合成参考文献
摘要:Zaidlewicz, M.; Pakulski, M. M., Science of Synthesis: Stereoselective Synthesis, (2011) 2, 65. 摘要:Johnson, J. B., Science of Synthesis: Stereoselective Synthesis, (2011) 3, 789.