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61.
J M Caba I M Rodriguez I Manzanares E Giralt F Albericio 《The Journal of organic chemistry》2001,66(23):7568-7574
Marine organisms are a rich source of novel, biologically active compounds. Herein, the solid-phase total synthesis of trunkamide A, currently in preclinical trials, is presented. Trunkamide A contains a thiazoline heterocycle and two residues of Ser and Thr with the hydroxy function modified as reverse prenyl (rPr). Cornerstones of the synthesis are as follows: (i) solid-phase peptide chain elongation using a quasi-orthogonal protecting scheme with tert-butyl and fluorenyl based groups, on a chlorotrityl resin; (ii) concourse of HOAt-based coupling reagents; and (iii) cyclizations in solution. Furthermore, the following synthetic steps are discussed: (i) preparation of the reverse prenyl derivatives of Ser and Thr; (ii) introduction of precursor of thiazoline as a protected amino thionoacid derivative; and (iii) formation of the thiazoline ring with DAST. All these features make this strategy particularly suitable for the large-scale synthesis of trunkamide A and other peptides containing the same motifs. 相似文献
62.
Skupinska KA McEachern EJ Skerlj RT Bridger GJ 《The Journal of organic chemistry》2002,67(22):7890-7893
A method to prepare amino-substituted 5,6,7,8-tetrahydroquinolines and 5,6,7,8-tetrahydroisoquinolines via catalytic hydrogenation of the corresponding acetamido-substituted quinolines and isoquinolines followed by acetamide hydrolysis is described. The yields of the products are good when the acetamido substituent is present on the pyridine ring and moderate with the acetamido substituent on the benzene ring. This method has also been applied to the regioselective reduction of quinoline substrates bearing other substituents (R = OMe, CO(2)Me, Ph). 相似文献
63.
64.
65.
Richard L. Martin Larry E. McMurchie Ernest R. Davidson 《International journal of quantum chemistry》1978,13(2):161-168
The completeness of a basis set for ethylene is examined relative to its ability to describe transition moments. The double zeta (Dunning contraction) plus polarization plus Rydberg Cartesian Gaussian set does much better for length than for velocity moments. An attempt is made to interpret the transition moment sums for the occupied orbitals. 相似文献
66.
The 13C NMR spectra of cyclobutane and seven methylated homologs and of ethyl cyclobutanecarboxylate and five isomeric diethyl cyclobutanedicarboxylates are reported and substituent parameters for methyl groups in methylcyclobutanes are calculated. Of note is a sizeable and nearly configuration-independent upfield shifting γ-effect. 相似文献
67.
Won Jei Cho Claude Bunel Ernest Marchal 《Journal of polymer science. Part A, Polymer chemistry》1980,18(6):1995-2000
Improved methods for the synthesis of 4-halogeno 1-vinylnaphthalenes are proposed. Reactivity ratios are determined for the following systems: 4-fluoro-1-vinyl naphthalene-styrene, 4-chloro-1-vinyl naphthalene-styrene, and 4-bromo-1-vinyl naphthalene-styrene. The determinations are performed at various specific temperatures and the relative activation parameters are obtained. It appears that the reactivity of 1-vinyl naphthalene is drastically decreased when substituted by a halogen. In the case of 1-vinyl naphthalene the selection is enthalpically controlled. 相似文献
68.
69.
Ernest Ma 《Physics letters. [Part B]》1976,65(5):468-470
A symmetric six-quark gauge model is proposed to account for the recent neutrino and antineutrino data on charged and neutral currents. As a bonus, exact isospin symmetry for strong interaction is obtained in a natural way. Further consequences are elaborated. 相似文献
70.
Ernest R. Ranucci 《School science and mathematics》1973,73(4):319-326