Sipak Joyasawal
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View article: Development of New Catalytic Asymmetric Routes towards a Cost-Driving Building Block of Nirmatrelvir
Development of New Catalytic Asymmetric Routes towards a Cost-Driving Building Block of Nirmatrelvir Open
Nirmatrelvir is an inhibitor of SARS-CoV-2 main protease and is the active ingredient in PaxlovidTM. Nirmatrelvir presents a significant synthetic challenge, in no small part due to a cost-driving lactam containing fragment with two stereo…
View article: CCDC 2246686: Experimental Crystal Structure Determination
CCDC 2246686: Experimental Crystal Structure Determination Open
An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available …
View article: Structure-property relationships of fluorinated carboxylic acid bioisosteres
Structure-property relationships of fluorinated carboxylic acid bioisosteres Open
Fluorinated alcohols and phenols are potentially useful as bioisosteres of the carboxylic acid functional group. To enable a direct comparison of the properties of fluorinated carboxylic acid surrogates with those of other commonly used, n…
View article: Conversion of α-Diazoketones into 1-Bromo-2-alkyl- or 2-arylpent-4-en-2-ols using Tin-Mediated Allylation/Propargylation
Conversion of α-Diazoketones into 1-Bromo-2-alkyl- or 2-arylpent-4-en-2-ols using Tin-Mediated Allylation/Propargylation Open
High-yielding and mild conditions are used to prepare of 1-bromo-2-alkyl- or 2-arylpent-4-en-2-ols/1-bromo-2-alkyl- or 2-arylpent-4-yn-2-ols from α-diazoketones. The reaction involves allylation/propargylation with successive bromide inser…
View article: Validation of HDAC8 Inhibitors as Drug Discovery Starting Points to Treat Acute Kidney Injury
Validation of HDAC8 Inhibitors as Drug Discovery Starting Points to Treat Acute Kidney Injury Open
Acute kidney injury (AKI), a sudden loss of kidney function, is a common and serious condition for which there are no approved specific therapies. While there are multiple approaches to treat the underlying causes of AKI, no targets have b…
View article: Challenges in the Highly Selective [3 + 1]-Cycloaddition of an Enoldiazoacetamide to Form a Donor–Acceptor Cis-Cyclobutenecarboxamide
Challenges in the Highly Selective [3 + 1]-Cycloaddition of an Enoldiazoacetamide to Form a Donor–Acceptor Cis-Cyclobutenecarboxamide Open
A substituted donor–acceptor cyclobutenecarboxamide is synthesized with modest enantiocontrol through a chiral copper(I) complex catalyzed [3 + 1]-cycloaddition reaction of α-acyl diphenylsulfur ylides with 3-siloxy-2-diazo-3-butenamides. …