Synthetic approaches to the 2011 new drugs

Ding, Hong X.; Liu, Kevin K.‐C.; Sakya, Subas M.; Flick, Andrew C.; O’Donnell, Christopher J

doi:10.1016/j.bmc.2013.02.061

Cited by 83 publications

(50 citation statements)

References 118 publications

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“…The halogenation of 76 was done with POCl 3 to obtain 77 in 80% yield. 117,[146][147][148][149] Compound 83, another key intermediate, was prepared in four steps from 3,5-dimethyl-4-aminobenzaldehyde (78). The amino group in 78 was protected as dimethylformamidine using N,N-dimethylformamide dimethyl acetal (79) to form 80 which was subsequently reacted with n-BuLi to give 81.…”

Section: Commercial Synthesis Of Rpvmentioning

confidence: 99%

The Journey of HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitors (NNRTIs) from Lab to Clinic

Vanangamudi²,

et al. 2018

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Human immunodeficiency virus (HIV) infection is now pandemic. Targeting HIV-1 reverse transcriptase (HIV-1 RT) has been considered one of the most successful targets for the development of anti-HIV treatment. Among the HIV-1 RT inhibitors, non-nucleoside reverse transcriptase inhibitors (NNRTIs) have gained a definitive place due to their unique antiviral potency, high specificity and low toxicity in antiretroviral combination therapies used to treat HIV. Till now, >50 structurally diverse classes of compounds have been reported as NNRTIs. Among them, six NNRTIs were approved for HIV-1 treatment, namely, nevirapine (NVP), delavirdine (DLV), efavirenz (EFV), etravirine (ETR), and rilpivirine (RPV), and doravirine (DOR). In this perspective, we focus on the six NNRTIs and lessons learned from their journey through development to clinical studies. It demonstrates the obligatory need of understanding the physicochemical and biological principles (lead optimization), resistance mutations, synthesis and clinical requirements for drugs.

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Section: Commercial Synthesis Of Rpvmentioning

confidence: 99%

The Journey of HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitors (NNRTIs) from Lab to Clinic

Vanangamudi²,

et al. 2018

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“…The IL was used in a molar ratio of 1:6 (reactant/IL), and it was recovered and reused three times with no appreciable decrease in yield. Dong [1,3]oxazine, however, in the presence of strong electron-withdrawing substituents such as m-, or p-NO 2 , no products were formed [275]. The authors cited that the reaction when carried out in THF as a molecular solvent, although afforded product in excellent yield, yet their separation from reaction mixture pose difficulty in compared to the reaction carried out using ILs [273].…”

Section: Oxazinesmentioning

confidence: 99%

Ionic Liquids-Prompted Synthesis of Biologically Relevant Five- and Six-Membered Heterocyclic Skeletons

Mishra

Kumar

Singh

et al. 2015

Green Synthetic Approaches for Biologically Relevant Heterocycles

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“…Ticagrelor 1 , as shown in Figure , is a platelet adenosine diphosphate (ADP) P2Y12 (P2T) reversible receptor antagonist for the treatment of patients with acute coronary syndromes (ACS). During the synthesis of Ticagrelor KSM ( 2 ) (Figure ), we encountered a significant problem of identifying mainly all the isomers as a pool of potential impurities.…”

Section: Introductionmentioning

confidence: 99%

Stereoselective Synthesis for Potential Isomers of Ticagrelor Key Starting Material

Madaraboina

Yakambaram

Pandey

et al. 2019

Journal of Heterocyclic Chem

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Tartrate salt of carbocyclic amine 2 is one of the key starting materials for the synthesis of Ticagrelor 1. During the synthesis of 1, the isomers of 2 also need to be considered as potential impurities and characterized before establishing the specification of product. In the present work, detailed study has been carried out to synthesize the related substances of 2, and their structure characterization has been discussed.

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Synthetic approaches to the 2011 new drugs

Cited by 83 publications

References 118 publications

The Journey of HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitors (NNRTIs) from Lab to Clinic

The Journey of HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitors (NNRTIs) from Lab to Clinic

Ionic Liquids-Prompted Synthesis of Biologically Relevant Five- and Six-Membered Heterocyclic Skeletons

Stereoselective Synthesis for Potential Isomers of Ticagrelor Key Starting Material

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