Synthesis of γ-oxo α-amino acids from L-aspartic acid
作者:Alexander S. Golubev、Norbert Sewald、Klaus Burger
DOI:10.1016/0040-4020(96)00942-8
日期:1996.11
of different γ-oxo α-amino acids from hexafluoroacetone protected L-aspartic acid chloride 1 via Stille cross coupling reaction is described. Stille reaction of 1 with vinyltributyltin followed by Lewis acid catalyzed intramolecular Michael addition provides access to 4-substituted pipecolicacidderivatives. An efficient synthesis of 5-hydroxy-4-oxo-L-norvaline 7 and a new approach to the 4-oxo-L-ornithine
Radiosynthesis and Evaluation of [18F]Selectfluor bis(triflate)
作者:Harriet Teare、Edward G. Robins、Anna Kirjavainen、Sarita Forsback、Graham Sandford、Olof Solin、Sajinder K. Luthra、Véronique Gouverneur
DOI:10.1002/anie.201002310
日期:2010.9.10
Selectfluor, one of the most reactive and commonly used electrophilic fluorinating N–F reagents, has been radiolabeled with 18F. The resulting new [18F]‐labeled N–F reagent is safe, nontoxic, and easy to handle. The combined use of [18F]Selectfluor bis(triflate) and AgOTf allows for the preparation of electron‐rich 18F‐aromatic compounds through a simple “shake and mix” protocol at room temperature
Bis mono- and bicyclic aryl and heteroaryl compounds which inhibit EGF
申请人:Rhone-Poulenc Rorer Pharmaceuticals Inc.
公开号:US05409930A1
公开(公告)日:1995-04-25
This invention relates to bis mono- and/or bicyclic aryl and/or heteroaryl compounds exhibiting protein tyrosine kinase inhibition activity. More specifically, it relates to the method of inhibiting abnormal cell proliferation in a patient suffering from a disorder characterized by such proliferation comprising the administration thereto of an EGF and/or PDGF receptor inhibiting effective amount of said bis mono- and/or bicyclic aryl and/or heteroaryl compound and to the preparation of said compounds and their use in pharmaceutical compositions used in this method.
Bis mono-and bicyclic aryl and heteroaryl compounds which inhibit EGF
申请人:Rhone-Poulenc Rorer Pharmaceuticals Inc.
公开号:US05656643A1
公开(公告)日:1997-08-12
This invention relates to bis mono- and/or bicyclic aryl and/or heteroaryl compounds exhibiting protein tyrosine kinase inhibition activity. More specifically, it relates to the method of inhibiting abnormal cell proliferation in a patient suffering from a disorder characterized by such proliferation comprising the administration thereto of an EGF and/or PDGF receptor inhibiting effective amount of said bis mono- and/or bicyclic aryl and/or heteroaryl compound and to the preparation of said compounds and their use in pharmaceutical compositions used in this method.
An efficient and convenient synthesis of enantiopure 4-(t-butyldimethylsilyloxy)-cyclohex-2-en-1-one: a formal synthesis of (±)-mesembranol
作者:Jerry B. Evarts、Philip L. Fuchs
DOI:10.1016/s0040-4039(01)00481-6
日期:2001.5
Inexpensive enantiopure (+)-limonene oxide 1 is converted to 4-(R)-(t-butyldimethylsilyloxy)-cyclohex-2-en-1-one 2a. All isolated intermediates can be distilled obviating the need for chromatography. With 2a,b in hand, a formal synthesis of (+/-)-mesembranol 17 using vinyl triflate methodology is high) yielding. (C) 2001 Elsevier Science Ltd. All rights reserved.