scholarly journals A Newfangled Synthesis of Integrase Inhibitor Drug Substance Raltegravir Potassium

2019 ◽  
Vol 31 (11) ◽  
pp. 2618-2622
Author(s):  
S. Venkat Rao ◽  
Vamsi Krishna Potluri ◽  
Ramesh Babu Potluri
Keyword(s):  
Integrase Inhibitor ◽  
Starting Material ◽  
Drug Substance ◽  
Synthetic Approach ◽  
Carbonyl Chloride ◽  
Stability Issue ◽  
Inhibitor Drug ◽  
Almost All

Raltegravir sodium synthesis was achieved from its one of the key starting materials with retro synthetic approach, in which without using its critical starting material chemically known as 5-methyl-1,3,4-oxadiazole-2-carbonyl chloride and which is more unstable during the synthesis of raltegravir potassium. Almost all the existed literatures commonly using this starting material in its synthesis even it is having a stability issue and hence to achieve a stable and economically viable synthesis. The current research describes a new route of synthesis by constructing an oxadiazole ring in a retro synthetic manner.

scholarly journals Synthesis of Novel Schiff Base Derivates Containing a Fragment of the HIV Integrase Inhibitor Drug Raltegravir

Proceedings ◽  
2019 ◽  
Vol 41 (1) ◽  
pp. 5
Author(s):  
Jairo J. Rojas-Ortiz ◽  
Claudia Contreras-Celedón ◽  
Mario A. Gómez-Hurtado ◽  
Luis Chacón-García ◽  
Carlos J. Cortes-García
Keyword(s):  
Schiff Base ◽  
Medicinal Chemistry ◽  
Nitrogen Heterocycles ◽  
Integrase Inhibitor ◽  
Hiv Integrase ◽  
First Report ◽  
Biological Relevance ◽  
Inhibitor Drug

An eco-friendly methodology for the synthesis of novel Schiff base analogs of Raltegravir, an Integrase inhibitor drug is described. Pertinence of these imine derivatives is related to Medicinal Chemistry to develop new anti-VIH compounds. To our knowledge, this is the first report of the synthesis of Schiff base using a Raltegravir drug fragment as amino component. In addition, these Imines will be used as a synthetic precursor to prepare other nitrogen heterocycles of biological relevance such as 1,5-disubstituted Tetrazoles.

scholarly journals From the Research on Risk Management in Polish Construction Enterprises

2019 ◽  
Vol 262 ◽  
pp. 07009 ◽  
Author(s):  
Józef Myrczek ◽  
Piotr Tworek
Keyword(s):  
Construction Industry ◽  
Synthetic Approach ◽  
Construction Sector ◽  
Construction Enterprises ◽  
Construction Companies ◽  
Financing Risk ◽  
Potential Risks ◽  
The Subject ◽  
Managing Risk ◽  
Almost All

A variety of insurance options are used when managing risk in the construction industry. Numerous insurers operating on the Polish market provide suitable types of insurance, thus allowing participants of a construction process to obtain a comprehensive cover against almost all potential risks. Therefore, ‘all-risks’ types of insurance is of particular importance in case of construction and assembly activities. In addition to this instrument, the paper also deals with other forms of insurance used in the construction sector in Poland, which apply to various aspects of activities conducted by actors involved a construction project. This is the main topic of the paper, which also outlines the theory on the subject as well as providing the results of empirical research carried out in this area and emphasizing the practical applicability of the discussions. Consequently, the key aim of the paper is to present the issues related to insurance in the construction industry as a method of financing risk in operations of construction companies. The paper adopts a synthetic approach to these issues. The paper also reviews the related scholarly literature.

scholarly journals Synthetic approach to the synthesis of eudesmane type of sesquiterpenes by using furan derivatives as a starting material.

1976 ◽  
Vol 24 (6) ◽  
pp. 1354-1361 ◽  
Author(s):  
TETSUJI KAMETANI ◽  
HIDEO NEMOTO ◽  
MIE TAKEUCHI ◽  
SATOSHI HIBINO ◽  
KEIICHIRO FUKUMOTO
Keyword(s):  
Starting Material ◽  
Synthetic Approach ◽  
Furan Derivatives

scholarly journals Identification, Isolation and Origin of Potential Dimer Impurities of Dichlorphenamide: A Carbonic Anhydrase Inhibitor Drug (Antiglaucoma)

2021 ◽  
Vol 33 (6) ◽  
pp. 1249-1252
Author(s):  
T. Purendar Reddy ◽  
Nageshwar Dussa ◽  
Srinivas Mamidi ◽  
Mahesh Panasa ◽  
Ramadas Chavakula ◽  
...  
Keyword(s):  
Carbonic Anhydrase ◽  
Drug Product ◽  
Carbonic Anhydrase Inhibitor ◽  
Drug Substance ◽  
Substantial Impact ◽  
Isolation And Characterization ◽  
New Process ◽  
Inhibitor Drug

Present work describes the identification, isolation and characterization of two new process related dimeric impurities of dichlorphenamide (1). During the synthesis of dichlorphenamide, the formation of two new dimeric impurities namely 2,3-dichloro-5-(3,4-dichloro-5-sulfamoyl-phenyl)sulfonylbenzenesulfonamide (2) (1,1Œ-dichlorphenamide dimer) and 2,3-dichloro-5-(2,3-dichloro-5-sulfamoylphenyl) sulfonyl-benzenesulfonamide (3) (1,3Œ-dichlorphenamide dimer) was observed. In addition, origin and the strategies adapted to control these potential dimer impurities were also described. These impurities have a substantial impact on the quality of the drug substance as well as drug product.

An improved and practical synthesis of Fmoc Rink linker

2019 ◽  
Vol 43 (3-4) ◽  
pp. 81-85
Author(s):  
Ling-yan Qin ◽  
Hao-ting Zhu ◽  
Li Zhan ◽  
Yong Zhu ◽  
Yu Luo
Keyword(s):  
Solid Phase Synthesis ◽  
Solid Phase ◽  
Scale Up ◽  
Starting Material ◽  
Synthetic Approach ◽  
Phase Synthesis ◽  
Practical Synthesis

Fmoc Rink linker is a widely used peptide-resin linker in the solid-phase synthesis of peptide-amides. This paper describes an improved and practical eight-step synthetic approach for this compound in a 50% overall yield, using p-hydroxybenzaldehyde as the starting material. The procedure is operationally simple and amenable to scale-up synthesis.

Assessing the Risk of Formation of Potential Genotoxic Degradation Products in a Small-Molecule Kinase Inhibitor Drug Substance and Drug Product

2015 ◽  
Vol 19 (11) ◽  
pp. 1458-1464 ◽  
Author(s):  
Mark A. Strege ◽  
Linda M. Osborne ◽  
Evan M. Hetrick ◽  
Allison L. Dill ◽  
Patrick J. Jansen ◽  
...  
Keyword(s):  
Small Molecule ◽  
Kinase Inhibitor ◽  
Degradation Products ◽  
Drug Product ◽  
Drug Substance ◽  
Small Molecule Kinase Inhibitor ◽  
Inhibitor Drug

scholarly journals A Multidisciplinary Investigation to Determine the Structure and Source of Dimeric Impurities in AMG 517 Drug Substance

2009 ◽  
Vol 2009 ◽  
pp. 1-12 ◽  
Author(s):  
Maria Victoria Silva Elipe ◽  
Zhixin Jessica Tan ◽  
Michael Ronk ◽  
Tracy Bostick
Keyword(s):  
Hplc Analysis ◽  
Scale Up ◽  
2D Nmr ◽  
Starting Material ◽  
Drug Substance ◽  
Synthetic Route ◽  
Stress Studies ◽  
Experimental Drug ◽  
Initial Scale

In the initial scale-up batches of the experimental drug substance AMG 517, a pair of unexpected impurities was observed by HPLC. Analysis of data from initial LC-MS experiments indicated the presence of two dimer-like molecules. One impurity had an additional sulfur atom incorporated into its structure relative to the other impurity. Isolation of the impurities was performed, and further structural elucidation experiments were conducted with high-resolution LC-MS and 2D NMR. The dimeric structures were confirmed, with one of the impurities having an unexpected C-S-C linkage. Based on the synthetic route of AMG 517, it was unlikely that these impurities were generated during the last two steps of the process. Stress studies on the enriched impurities were carried out to further confirm the existence of the C-S-C linkage in the benzothiazole portion of AMG 517. Further investigation revealed that these two dimeric impurities originated from existing impurities in the AMG 517 starting material, N-acetyl benzothiazole. The characterization of these two dimeric impurities allowed for better quality control of new batches of the N-acetyl benzothiazole starting material. As a result, subsequent batches of AMG 517 contained no reportable levels of these two impurities

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