Pharmablock (nanjing) R&d Co. Ltd

Tianyi Bioscience Co., Ltd.

Xihan Wu

Minmin Yang

Jin Li

Yurong Wang

Qingning Shu

Chunrui Zhu

Liwu Fu

Dongmei Zhang

Xiaoyu Yang

Jingwei Zhu

Disclosed are a pyrrolo[2,1-f][1,2,4]triazine derivative of Formula (I) and use thereof for treating tumors. The compound has remarkable antiproliferative activity for a variety of human tumor cell lines, and is useful for treating cancers, especially solid tumors such as gastric cancer, lung cancer, liver cancer, breast cancer, colon cancer, prostatic cancer, and oral cancer.

Pyrrolo[2, 1-F] [1,2,4]triazine derivative and use thereof for treating tumors

The present invention relates to the field of pharmaceutical chemistry, and particularly to an aza-benzo[f]azulen derivative (I) and an antitumor effect thereof. Pharmacological tests show that the compound of the present invention has in vitro and in vivo antitumor activities, and can be developed into clinical drugs for treating or controlling diseases such as stomach cancer, lung cancer, liver cancer, breast cancer, colon cancer, prostate cancer, and oral cancer.

Antitumor aza-benzo [f] azulen derivative, method for preparing same, and use thereof

The present invention relates to the field of chemical synthesis, and in particular to a method for synthesizing 1-(2-fluorobenzyl)-1H-pyrazolo[3,4-b]pyridin-3-formamidine hydrochloride, which is an important intermediate of Riociguat that is an anti-thromboembolic-disease medicine. The method is characterized in that: 3-iodo-1H-pyrazolo[3,4-b]pyridine is used as a raw material; the raw material is reacted with fluorobenzyl bromide to form a compound (10); the compound (10) is reacted with zinc cyanide to form a compound (6); the compound (6) is reacted with sodium methoxide, ammonium chloride, acetic acid and methanol to form a compound (8); and the compound (8) is reacted with chlorine hydride gas to form 1-(2-fluorobenzyl)-1H-pyrazolo[3,4-b]pyridin-3-formamidine hydrochloride. The method has the characteristics of cheap and readily available raw materials, high yield, mild reaction conditions and the like, and is a synthesis method having a large-scale preparation value.

Method for synthesizing 1-(2-fluorobenzyl)-1H-pyrazolo[3,4-b]pyridine-3-formamidine hydrochloride

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Jiangsu, China

Xihan Wu