38870-89-2Relevant articles and documents
A Diels-Alder reaction for the total synthesis of the novel antibiotic antitumor agent mensacarcin
Tietze, Lutz F.,Guentner, Carlos,Gericke, Kersten M.,Schuberth, Ingrid,Bunkoczi, Gabor
, p. 2459 - 2467 (2005)
The antibiotic mensacarcin (1), which contains nine stereogenic centers and two epoxy functionalities, is a novel antitumor agent that was first isolated from the culture broth of Streptomyces sp. Goe C4/4 found in a soil sample next to the northern cafeteria of the University of Goettingen. For the synthesis of 1 and related structurally simplified analogs, a Diels-Alder reaction of O-methyljuglone (11) and the tetra-substituted 1,3-butadiene 22 was performed to give the cycloadduct rac-28, which was transformed into the epoxides rac-31 and rac-33. The cytotoxicity of rac-33 is only 53 times lower than the much more complex 1. Wiley-VCH Verlag GmbH & Co. KGaA, 69451 Weinheim, Germany, 2005.
Preparation method and application of iopromide intermediate (by machine translation)
-
Paragraph 0056-0058, (2020/07/24)
The invention relates to a preparation method of an iopromide intermediate and an application thereof in preparation of iopromide. The method comprises the following steps: compound VI compound is subjected to reduction reaction under the action of Raney nickel/hydrazine hydrate to obtain the compound V compound. The reaction is carried out under normal pressure, the operation is simple and safe, the generated intermediate impurities are less, and the reaction is more suitable for industrial production. The method is used for preparing iopromide, can avoid the generation of a diacylated by-product, can effectively reduce the generation of by-products in the preparation process, can be easily separated and purified, and can obtain high-purity iopromide with high yield. (by machine translation)
Synthesis and application of peptide borate compounds
-
Paragraph 0163; 0179-0181, (2019/12/25)
The invention belongs to the field of drug synthesis, and specifically relates to a series of novel peptide borate compounds or pharmaceutical salts thereof, and a preparation method and pharmaceutical application thereof. The structure of the peptide borate compounds or the pharmaceutical salts thereof is as shown in a formula I which is described in the specification. The compounds of the invention can be used for preparing proteasome inhibitors, and thus can be further used for treating solid tumors and blood tumors.