Synlett 2024; 35(17): 2027-2031
DOI: 10.1055/s-0042-1751579
letter

TfOH-Catalyzed Facile Access for One-Pot Synthesis of β-Acylamino Ketones by Avoiding the Usage of Acetyl Chloride

Sachin D. Kharat
a   Department of Chemistry, & Central Research Laboratory ASC College, Indapur, Dist-Pune, 413106, India
b   Department of Chemistry, PDEA’s Baburaoji Gholap College, Sangvi Pune, 411 027, India
,
Prasad B. Rupnavar
c   Department of Chemistry, MES Abasaheb Garware College, Pune, 411 004, India
,
Keshav S. Pakhare
d   Department of Chemistry, Anandibai Raorane Arts, Commerce and Science College, Vaibhavwadi, Dist-Sindhudurg, 416810, India
,
Ayesha A. Khan
e   Department of Chemistry, Savitribai Phule Pune University, Pune, 411007, India
,
Bapurao D. Rupanawar
f   Chemistry and Chemical Bioengineering Unit, Okinawa Institute of Science and Technology Graduate University, 1919-1 Tancha, Onna, Okinawa, 904-0495, Japan
,
Mahadev P. Shinde
a   Department of Chemistry, & Central Research Laboratory ASC College, Indapur, Dist-Pune, 413106, India
b   Department of Chemistry, PDEA’s Baburaoji Gholap College, Sangvi Pune, 411 027, India
› Author Affiliations


Abstract

We have developed a TfOH-catalyzed, highly efficient protocol for the synthesis of biologically active β-acylamino ketones from aldehyde, ketone, and nitrile by avoiding the use of acetyl chloride. The reaction proceeds through a sequential aldol reaction followed by a nucleophilic attack of nitrile and hydrolysis of nitrile in one pot. The attractive features of this tandem process are mild reaction conditions, high atom economy, broad substrate scope with 51–87% yield, gram-scale reaction, and ease of operation.

Supporting Information



Publication History

Received: 23 November 2023

Accepted after revision: 18 March 2024

Article published online:
28 March 2024

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