Microwave-assisted efficient and convenient synthesis of 2,4(1H,3H)-quinazolinediones and 2-thioxoquinazolines.
An efficient and convenient method was developed for the preparation of 2,4(1H,3H)-quinazolinediones and 2-thioxoquinazolinones. Substituted methyl anthranilate reacted with various iso(thio)cyanates in DMSO/H2O without any catalyst or base by using microwave irradiation to generate diversity on the 2,4(1H,3H)-quinazolinediones or 2-thioxoquinazolinones. A variety of substrates can participate in the process with good yields and high purities, making this methodology suitable for library synthesis in drug discovery efforts.
Li
Zhaoguang
Z
Drug Discovery and Design Centre, State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Shanghai Institutes for Biological Sciences, Chinese Academy of Sciences, 555 Zuchongzhi Road, Shanghai 201203, China.
Huang
He
H
Sun
Hongbin
H
Jiang
Hualiang
H
Liu
Hong
H
D020650:Combinatorial Chemistry Techniques; D008872:Microwaves; D015394:Molecular Structure; D011799:Quinazolines / Q000138:chemical synthesis* / Q000737:chemistry / Q000528:radiation effects*; D013237:Stereoisomerism
D011799:Quinazolines; C081989:2,4(1H,3H)-quinazolinedione