200356-31-6Relevant academic research and scientific papers
Additive Tuned Selective Synthesis of Bicyclo[3.3.0]octan-1-ols and Bicyclo[3.1.0]hexan-1-ols Mediated by AllylSmBr
Wang, Xiaoxia,Li, Jianyong,Yuan, Ting,You, Bingxin,Xie, Guanqun,Lv, Xin
, p. 8984 - 8994 (2018/07/05)
The selective construction of bicyclo[3.3.0]octan-1-ols and bicyclo[3.1.0]hexan-1-ols was achieved by using an allylSmBr/additive(s) system. By employing HMPA as the only additive, the momoallylation/ketone-alkene coupling occurred preferably and afforded bicyclo[3.3.0]octan-1-ols in good yields with high diastereoselectivities. While the ester-alkene coupling predominated to generate bicyclo[3.1.0]hexan-1-ols in moderate yields with excellent diastereoselectivities in the presence of a proton source, such as pyrrole as the coadditive with HMPA. The tunable reactivity of allylSmBr by additive(s) would make it a versatile reagent in organic synthesis.
HETEROARYL DERIVATIVES AS SEPIAPTERIN REDUCTASE INHIBITORS
-
Paragraph 001095, (2017/05/31)
Inhibitors of sepiapterin reductase of formula (I) or (I'), wherein the substituents are defined as in the claims, and uses of sepiapterin reductase inhibitors in analgesia, treatment of acute and chronic pain, anti-inflammation, and immune cell regulation are disclosed.
AMINOQUINAZOLINE DERIVATIVES AND THEIR SALTS AND METHODS OF USE
-
, (2014/08/19)
The present invention relates to the field of medicine. Provided herein are aminoquinazoline derivatives, their salts and pharmaceutical formulations useful in modulating the protein tyrosine kinase activity, and in modulating inter- and/or intra-cellular signaling. Also provided herein are pharmaceutically acceptable compositions comprising the aminoquinazoline compounds and methods of using the compositions in the treatment of hyperproliferative disorders in mammals, especially humans.
AMINOQUINAZOLINE DERIVATIVES AND THEIR SALTS AND METHODS OF USE
-
, (2013/06/05)
The present invention relates to the field of medicine. Provided herein are aminoquinazoline derivatives, their salts and pharmaceutical formulations useful in modulating the protein tyrosine kinase activity, and in modulating inter-and/or intra-cellular signaling. Also provided herein are pharmaceutically acceptable compositions comprising the aminoquinazoline compounds and methods of using the compositions in the treatment of hyperproliferative disorders in mammals, especially humans.
Lewis Acid Mediated [2,3]-Sigmatropic Rearrangement of Allylic α-Amino Amides
Blid, Jan,Brandt, Peter,Somfai, Peter
, p. 3043 - 3049 (2007/10/03)
Boron trifluoride and BBr3 mediated [2,3]-sigmatropic rearrangements of allylic α-amino amides have been developed affording secondary amines in good yields. (E)-Crotyl and (E)-cinnamyl α-amino amides 2b and 2c exhibit excellent syn-diastereoselectivity upon rearrangement with either Lewis acid. The allylic amine 2a forms upon treatment with BF 3 or BBr3 a five-membered heterocylic complex in which a single halide anion has been displaced by the carbonyl oxygen atom. The structures of the Lewis acid-amine complexes were elucidated using NMR spectroscopy. A plausible reaction mechanism, based on DFT calculations, is presented. Thus, BF3- or BBr3-complexed allylic amines 2 are shown to preferentially proceed, after deprotonation, via an endo transition state.
Investigations into the [2,3]-aza-Wittig rearrangement of N-alkyl N-allyl α-amino esters
Coldham, Iain,Middleton, Mark L.,Taylor, Philip L.
, p. 2817 - 2821 (2007/10/03)
A Lewis acid is needed in order to allow the [2,3]-sigmatropic rearrangement of N-alkyl N-allyl α-amino esters to give rise to N-alkyl C-allyl glycine esters. Addition of iodomethane, rather than a Lewis acid, promotes quaternary ammonium salt formation, in situ ylide formation and [2,3]-sigmatropic rearrangement to N,N-dialkyl C-allyl glycine esters.
