Efficient and Convenient Synthesis of N3-(Acyloxymethyl)dihydropyrimidinones by a One-Pot Two-Step Method
3,4-Dihydropyrimidinones modified with N3-(acetoxymethyl) and (aroyloxymethyl) groups can be regioselectively obtained in good yields by reactions of 3,4-dihydropyrimidinones with paraformaldehyde and substituted benzoic acids/acetic acid, by a one-pot two-step strategy in the presence of chlorotrimethylsilane. The advantages of this method are the simple procedure, the high regioselectivity of the products, shorter reaction time and the mild reaction conditions. Additionally, this method directly uses acid as acylation reagents and needs not acid anhydride or acyl chloride.
Keywords: 3,4-dihydropyrimidinones; Biginelli compounds; DHPM; N-alkylation; N3-(Acetoxymethyl)dihydropyrimidinones; N3-(benzoyloxymethyl)dihydropyrimidinones; adrenergic; antihypertensives; cyclocondensation; one-pot reaction
Document Type: Research Article
Publication date: 01 March 2011
- Letters in Organic Chemistry publishes original letters on all areas of organic chemistry including synthesis, bioorganic, medicinal, natural products, organometallic, supramolecular, molecular recognition and physical organic chemistry. The emphasis is placed on publishing quality papers very rapidly. Letters are processed rapidly and take full advantage of the Internet technology both for the submission and the review of the manuscripts.
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