133909-99-6Relevant articles and documents
Trityl losartan
Sieron, Leslaw,Nagaraj,Prabhuswamy,Yathirajan,Nagaraja,Narasegowda,Gaonkar
, p. o821-o823 (2004)
The title compound (systematic name: (2-butyl-4-chloro-1-[2-(2-trityl-2H- tetrazol-5-yl)biphenyl-4-ylmethyl]-1H-imidazol-5-yl}methanol), C 41H37ClN6O, crystallizes in the centrosym-metric space group P1 with two independent molecules in the asymmetric unit. These molecules differ significantly only in the relative orientations of the rings in the biphenylyltetrazole moieties. One of the molecules shows disorder for three C atoms in the n-butyl group. Hydrogen bonds link the molecules in an infinite chain along the a axis.
Continuous Synthesis and Separation ofp-Bromobenzyl Bromide Using Atom-Efficient Bromination ofp-Bromotoluene without Any Organic Effluent: Potential for Green Industrial Practice
Sancheti, Sonam V.,Yadav, Ganapati D.
, p. 2071 - 2080 (2021/09/13)
This work focuses on the bromination ofp-bromotoluene (PBT) using different brominating agents such as liquid Br2, NaBr-NaBrO3, NaBr-NaBrO3-NaCl, NaBr-H2O2, and HBr-H2O2. NaBr-NaBrO3-NaCl is an eco-friendly brominating agent obtained from a bromine recovery plant. Both NaBr-NaBrO3and NaBr-NaBrO3-NaCl were found to be nonhazardous and efficient brominating agents. Pure NaBr-NaBrO3resulted in the best PBT conversion with 79.7% Br atom efficiency in water and 98.2% average Br atom efficiency using dichloroethane as a solvent. Dichloroethane is de facto no longer used in the US and Europe and is not eco-friendly; the process with water as a solvent is the best. The substrate to active bromine molar ratio of 3:1 was found to be sufficient to get the maximum selectivity ofp-bromobenzyl bromide (PBBB). The low-temperature crystallization method was used for separation cum purification of the product. Unreacted PBT was recycled along with the dibromo byproduct obtained. The dibromo product, which was built up gradually in the reaction mixture over 10 successive batches, was converted back into PBBB/PBT through NaBH4treatment of the mother liquor. This continuous process is highly sustainable and produces zero organic waste, making it potentially attractive toward green industrial implementation.
New losartan-hydrocaffeic acid hybrids as antihypertensive-antioxidant dual drugs: Ester, amide and amine linkers
García, Gonzalo,Serrano, Isabel,Sánchez-Alonso, Patricia,Rodríguez-Puyol, Manuel,Alajarín, Ramón,Griera, Mercedes,Vaquero, Juan J.,Rodríguez-Puyol, Diego,álvarez-Builla, Julio,Díez-Marqués, María L.
experimental part, p. 90 - 101 (2012/07/13)
We report new examples of a series of losartan-hydrocaffeic hybrids that bear novel ester, amide and amine linkers. These compounds were made by linking hydrocaffeic acid to the side chain of losartan at the C-5 position of the imidazole ring through different strategies. Experiments performed in cultured cells demonstrate that these new hybrids retain the ability to block the angiotensin II effect and have increased antioxidant ability. Most of them reduced arterial pressure in rats better or as much as losartan.
A process for the preparation of losartan derivatives by chlorination and reduction of the respective 1H-imidazole-5-carbaldehydes
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Page/Page column 11, (2008/06/13)
The invention provides a process for the preparation of a sartan derivative of formula (I): wherein R = C2-C7 straight or branched alkyl or C3-C9 cycloalkyl, or a pharmaceutically acceptable salt thereof, comprising the steps of chlorinating and reducing, in any order, a compound of formula (III): wherein R is defined as above to form a compound of formula (VI), wherein R is defined as above and then deprotecting said compound of formula (VI) to obtain the sartan derivative of formula (I), and optionally converting said sartan derivative into one of its pharmaceutically acceptable salts. A preferred embodiment of this invention is a process for the preparation of losartan and, particularly, its potassium salt.