114812-34-9Relevant articles and documents
Exploring steric effects in diastereoselective synthesis of chiral aminophenolate zinc complexes and stereoselective ring-opening polymerization of rac-lactide
Wang, Haobing,Yang, Yang,Ma, Haiyan
supporting information, p. 7356 - 7372 (2016/08/06)
A series of tridentate chiral aminophenol proligands and corresponding zinc complexes, LZnX (L = (S)-2-{[(1-R4-2-pyrrolidinyl)CH2N(R3)-]CH2}-6-R1-4-R2-C6H2O, X = N(SiMe3)2, R3 = nBu, R4 = Bn: R1 = R2 = Cl (1), R1 = R2 = Me (2), R1 = R2 = tBu (3); X = N(SiMe3)2, R1 = trityl, R2 = Me: R3 = n-octyl, R4 = Bn (4), R3 = Bn, R4 = Bn (5), R3 = nBu, R4 = naphthalen-1-ylmethyl (6), R3 = nBu, R4 = iPr (7); R1 = R2 = cumyl, R3 = Et, R4 = Bn: X = N(SiMe3)2 (8), X = OtBu (9), X = Et (10), X = Cl (11)), have been synthesized. Complexes 4, 6, and 11 were obtained as enantiopure products (4 and 6 as enantiopure a; 11 as enantiopure b), while complexes 1-3, 5, and 7-10 as a pair of diastereomers, but in different ratios, which have been proved by X-ray diffraction and NMR spectroscopic studies. When exposed to the ring-opening polymerization of rac-lactide, most of these complexes can effectively produce PLAs with narrow polydispersities, desirable molecular weights, and moderate to high isotacticities. The structure-selectivity relationships, including the relationships of structure-synthesis diastereoselectivity and structure-polymerization stereoselectivity, have been further investigated. Consistent trends of diastereoselectivity and stereoselectivity are observed with the variations of the R1 group at the ortho-position of the phenolate ring and the R3 group in the pyrrolidinyl moiety. The decrease of the steric bulkiness of the R4 group on the central amine has less influence on the diastereoselectivity, but leads to considerable loss of the stereoselectivity, whereas the decrease of the steric bulkiness of the X group results in a reverse of the diastereoselectivity, but shows no influence on the stereoselectivity. There is probably no direct relationship between the diastereoselectivity in complex synthesis and the stereoselectivity of the complex toward the ROP of rac-LA. The stereocontrol of these complexes might largely rely on the substituents in the ligand framework rather than their diastereomer ratios.
COMPOUNDS USEFUL AS INHIBITORS OF ATR KINASE
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Page/Page column 190, (2010/06/11)
The present disclosure relates to pyrazine compounds of formula (I) wherein L, n, R1, and R2 are as described in the specification. These compounds are useful as inhibitors of ATR protein kinase. The disclosure also relates to pharmaceutically acceptable compositions comprising the compounds of the disclosure; methods of treating of various diseases, disorders, and conditions using the compounds of the disclosure; processes for preparing the compounds of the disclosure; intermediates for the preparation of the compounds of the disclosure; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors.
N-Fluoroalkylated and N-Alkylated Analogues of the Dopaminergic D-2 Receptor Antagonist Raclopride
Lannoye, G. S.,Moerlein, S. M.,Parkinson, D.,Welch, M. J.
, p. 2430 - 2437 (2007/10/02)
A series of raclopride -1-ethylpyrrolidine> derivatives bearing pyrrolidino N-fluoroalkyl or -alkyl substituents were synthesized and evaluated as potential dopaminergic receptor-based positron tom
