Organic nitriles are converted into cyanide ions through the action of cytochrome P450 enzymes in the liver. Cyanide is rapidly absorbed and distributed throughout the body. Cyanide is mainly metabolized into thiocyanate by either rhodanese or 3-mercaptopyruvate sulfur transferase. Cyanide metabolites are excreted in the urine. (L96)
Organic nitriles decompose into cyanide ions both in vivo and in vitro. Consequently the primary mechanism of toxicity for organic nitriles is their production of toxic cyanide ions or hydrogen cyanide. Cyanide is an inhibitor of cytochrome c oxidase in the fourth complex of the electron transport chain (found in the membrane of the mitochondria of eukaryotic cells). It complexes with the ferric iron atom in this enzyme. The binding of cyanide to this cytochrome prevents transport of electrons from cytochrome c oxidase to oxygen. As a result, the electron transport chain is disrupted and the cell can no longer aerobically produce ATP for energy. Tissues that mainly depend on aerobic respiration, such as the central nervous system and the heart, are particularly affected. Cyanide is also known produce some of its toxic effects by binding to catalase, glutathione peroxidase, methemoglobin, hydroxocobalamin, phosphatase, tyrosinase, ascorbic acid oxidase, xanthine oxidase, succinic dehydrogenase, and Cu/Zn superoxide dismutase. Cyanide binds to the ferric ion of methemoglobin to form inactive cyanmethemoglobin. (L97)
来源:Toxin and Toxin Target Database (T3DB)
毒理性
致癌物分类
对人类无致癌性（未列入国际癌症研究机构IARC清单）。
No indication of carcinogenicity to humans (not listed by IARC).
[EN] PROCESS FOR PREPARING (S)-TETRAHYDRO-A-(1-METHYLETHYL)-2-OXO-1(2H)- PYRIMIDINEACETIC ACID<br/>[FR] PROCEDE DE PREPARATION D'ACIDE ACETIQUE (S)-TETRAHYDRO-A-(1-METHYLETHYL)-2-OXO-1(2H)-PYRIMIDINE
申请人：CLARIANT LSM ITALIA SPA
公开号：WO2003101971A1
公开（公告）日：2003-12-11
A process for preparing (S)-tetrahydro-a-(1-methylethyl)-2-oxo-1(2H)-pyrimidineacetic acid, an intermediate that is useful in the synthesis of HIV protease inhibitors such as, for example, those described in US-5 914 332, is described.The process under consideration comprises the following steps:- L-valine is reacted with acrylonitrile;- the N-(2-cyanoethyl)-L-valine thus obtained is isolated and then reacted with an alkyl chloroformate;- the N-(2-cyanoethyl)-N-(alkoxycarbonyl)-L-valine thus obtained is hydro-genated in the presence of a hydrogenation catalyst, preferably rhodium;- the N-(3-aminopropyl)-N-(methoxycarbonyl)-L-valine thus obtained is cyclized to give the desired compound.
Process for preparing (s)-tetrahydro-a-(1-methylethyl)-2-oxo-1(2h)-pyrimidineacetic acid
申请人：Bertolini Giorgio
公开号：US20050222184A1
公开（公告）日：2005-10-06
A process for preparing (S)-tetrahydro-a-(1-methylethyl)-2-oxo-1(2H)-pyrimidineacetic acid, an intermediate that is useful in the synthesis of HIV protease inhibitors such as, for example, those described in U.S. Pat. No. 5,914,332, is described. The process under consideration comprises the following steps:—L-valine is reacted with acrylonitrile;—the N-(2-cyanoethyl)-L-valine thus obtained is isolated and then reacted with an alkyl chloroformate;—the N-(2-cyanoethyl)-N-(alkoxycarbonyl)-L-valine thus obtained is hydro-genated in the presence of a hydrogenation catalyst, preferably rhodium;—the N-(3-aminopropyl)-N-(methoxycarbonyl)-L-valine thus obtained is cyclized to give the desired compound.
申请人：Chia Tai Tianqing Pharmaceutical Group Co., Ltd.
公开号：EP3663299A1
公开（公告）日：2020-06-10
A bicyclic compound acting as a RORγ inhibitor. Provided are a compound of formula (I) or a pharmaceutically acceptable salt thereof, the compound having a structure as represented by formula (I-A) or formula (I-B). The provided compound of formula (I-A) or formula (I-B) or pharmaceutically acceptable salt thereof has good RORγ inhibitory activities, being expected to be used for treating diseases mediated by RORγ receptors in a mammal.
