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1.
A two-step protocol for the first chemoselective cleavage of 2-hydroxy acid amides has been developed. Mesylation of the model substrate 2-(hydroxypropionylamino)-4-methylpentanoic acid methyl ester (11) followed by treatment with N-ethylthiourea (13) allows cleavage of 2-hydroxy acid amides under smooth conditions. Successful application of this methodology to the open-chain transesterification product 15 (methylester) of the cyclic heptadepsipeptide HUN-7293, a potent inhibitor of inducible cell adhesion molecule expression, delivered the corresponding hexapeptide 18 with unprotected N-terminus in 70-75% yield. This result demonstrates that the protocol developed even works in the presence of an ester and several methylated and unmethylated amide bonds. Finally, a sequence of ligation of methyl D-dehydroglutaminate (20) to the C-terminus of the saponification product 21, followed by the degradation protocol and ring closure, allowed chemical "point mutation" at the DGCN site affording the aza analogue of HUN-7293 (24) in 15% overall yield. To the best of our knowledge this is the first report on chemoselective cleavage of 2-hydroxy acid amides. 相似文献
2.
Ernst Schaumann Erwin Kausch Karl-Heinz Klaska Rolf Klaska Otto Jarchow 《Journal of heterocyclic chemistry》1977,14(5):857-860
The crystal and molecular structures of the cycloadduct from isopropyl[α-(dimethylthio-carbamoyl)isopropyl]carbodiimide and methyl isothiocyanate were determined by single-crystal X-ray methods. The product was established to be 2-(1-isopropyl-3,5-dimethyl-4,6-dithioxo-hexahydro-1,3,5-triazine-2-ylidenamino)-N,N-dimethylthioisoburyramide, in which contrary to expectations based on hybridisation the heterocyclic ring adopts a boat conformation. 相似文献
3.
Erwin Mues 《manuscripta mathematica》1978,23(4):325-341
In this paper it is discussed for which entire functions g the homogeneous differential polynomial gg-ag2 has no zeros. It is shown that g(z)=exp (z+) are the only transcendental entire functions with this property if a1. The case a=1 is indeed exceptional. This result settles a question of Hayman. 相似文献
4.
Erwin Brüning 《Communications in Mathematical Physics》1978,58(2):167-194
The problem of uniqueness of monotone continuous linear extensions of $$T_{(2N)} = \{ 1,T_1 ,...,T_{2N} \} \in E'_{(2N)} = \prod\limits_{n = 0}^{2N} {E'_n } $$ is solved. A characterization of a relativistic QFT in terms of finitely many VEV's is derived. All results are illustrated by an explicit discussion of the extension problem for special cases ofT (4)={1,0,T 2,T 3,T 4}. This discussion contains explicitly necessary and sufficient conditions onT (4) for the existence of minimal extensions and some convenient sufficient conditions. 相似文献
5.
K[AlH(CH3)3] is formed by decomposition of K[Al(CH3)3SiH3] in diethyl ether. The compound crystallizes in the orthorhombic space group Cmca with the lattice parameters a = 9.647, b = 17.332, c = 7.711 Å. There are eight formula units in the unit cell. Analogously to K[Al(CH3)4] the hydrido compound contains isolated anions with a tetrahedral coordination of aluminium by hydrogen and three methyl groups. 相似文献
6.
Peter Rogl Subhash K. Naik Erwin Rudy 《Monatshefte für Chemie / Chemical Monthly》1977,108(5):1189-1211
The system TiC?HfC?WC was investigated by means of melting point, differential thermoanalytical, X-ray diffraction and metallographic techniques on hot pressed and heat treated as well as melted alloy specimens and a complete constitutional diagram from 1500°C through the melting range established. According to the peritectic melting of hexagonal WC both isopleths, TiC?WC as well as HfC?WC show a class II reaction at 2760°C in Ti?W?C and at 2730°C in Hf?W?C. The phase behaviour within the TiC?HfC?WC system is characterized by the presence of a (binary) miscibility gap within TiC?HfC [T c=1780°C, (TiC)0.55(HfC)0.45] which extends into the ternary forming a closed ternary miscibility gap at higher temperatures with an isolated ternary critical point:T c=1800°C, (TiC)0.55(HfC)0.45(WC)0.05. Interaction of the solvus (boundary of the cubic-B 1 monocarbide solid solution) and the ternary miscibility gap was established at 1540°C and (TiC)0.27(HfC)0.41(WC)0.32: Alloys of this composition enter a decomposition reaction on cooling into two isotypic cubic B 1 phases and hexagonal WC. Isothermal sections were calculated assuming regular solutions. 相似文献
7.
Julien Warnan Erwin Reisner 《Angewandte Chemie (International ed. in English)》2020,59(40):17344-17354
From the understanding of biological processes and metalloenzymes to the development of inorganic catalysts, electro‐ and photocatalytic systems for fuel generation have evolved considerably during the last decades. Recently, organic and hybrid organic systems have emerged to challenge the classical inorganic structures through their enormous chemical diversity and modularity that led earlier to their success in organic (opto)electronics. This Minireview describes recent advances in the design of synthetic organic architectures and promising strategies toward (solar) fuel synthesis, highlighting progress on materials from organic ligands and chromophores to conjugated polymers and covalent organic frameworks. 相似文献
8.
9.
We present experimental evidence for the spontaneous formation of a macroscopic spin polarization in overlapping regions of two independent Bose-Einstein condensates produced in different hyperfine states of 87Rb. The condensates are independent in the sense that we do not explicitly introduce a relative phase between them. A single "spin-tip" pulse maps the transverse spin polarization into longitudinal spin polarization, and the atomic density distributions are measured with a Stern-Gerlach imaging method. The resulting matter-wave interference patterns are anticorrelated. 相似文献
10.