13255-50-0Relevant articles and documents
Introduction of Z-GP scaffold into procarbazine reduces spermatoxicity and myelosuppression
Wang, Rikang,Zhang, Chao,Zheng, Chaojun,Li, Huilan,Xie, Xinshu,Jin, Yi,Liu, Zhijun,Chen, Heru
, p. 461 - 467 (2019)
Incorporation of carbobenzoxy-glycylprolyl (Z-GP) to either α or β position of the hydrazine moiety in procarbazine (Pcb) has been carried on in 5-steps process. The overall yield was 32.7%. The new entity Z-GP-Pcb was confirmed targeting to fibroblast activation protein-α (FAPα). Z-GP-Pcb may be hydrolyzed by either isolated rhFAPα or tumor homogenate. It was shown far less cytotoxicity against NCI-H460 cell line than Pcb. Z-GP-Pcb was displayed the potency to reduce spermatoxcity in H22-bearing mice. The mechanism may be ascribed to the blockade of dehydrogenation by α-glycerolphosphate dehydrogenase. This candidate was further proved equal antitumor activity to Pcb. However, the introduction of Z-GP scaffold decreased myelosuppression. All the evidences support that Z-GP-Pcb is a better antitumor agent than Pcb.
Synthetic method of procarbazide hydrochloride intermediate
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, (2020/05/14)
The invention discloses a synthetic method of a procarbazide hydrochloride intermediate. The preparation method comprises the following step: in a solvent, in the presence of a hydrolysis agent, carrying out hydrolysis reaction as shown in the specification on a compound as shown in a formula II to obtain a compound as shown in a formula I. The preparation method disclosed by the invention has theadvantages of high yield, high purity and stable process, and is suitable for industrial production.
Tf2O-Mediated Intermolecular Coupling of Secondary Amides with Enamines or Ketones: A Versatile and Direct Access to β-Enaminones
Liu, Yong-Peng,Zhu, Cheng-Jie,Yu, Cun-Cun,Wang, Ai-E,Huang, Pei-Qiang
supporting information, p. 7169 - 7174 (2019/11/16)
Based on the Tf2O-mediated intermolecular reaction of secondary amides with enamines derived from ketones, a novel approach to β-enaminones has been developed. The reaction is widely functional group tolerant and highly chemoselective. In the presence of 4 ? molecular sieves, the method can be extended to the one-pot condensation of secondary amides with ketones for NH β-enaminones synthesis.