Lithium-Acetate-Mediated Biginelli One-Pot Multicomponent Synthesis under Solvent-Free Conditions and Cytotoxic Activity against the Human Lung Cancer Cell Line A549 and Breast Cancer Cell Line MCF7

Table 2

Physical characterization data of compounds.^a

Compound	R	R^1	R^2	X	PPA Yield (%)	LiAc Yield (%)	M.P. (°C)
							Found	Reported
1	H	OEt	H	O	94	90	198–202	202-203 [25]
2	H	OEt	H	S	88	85	202–204	204–206 [25]
3	4-OCH3	OEt	H	O	93	91	205–207	199-200 [25]
4	4-OH	OEt	H	O	87	82	224–226	232–234 [25]
5	2-OH	OEt	H	O	85	80	195–200	201–203 [25]
6	3-OH	OEt	H	O	78	81	161–163	163–165 [26]
7	4-Cl	OEt	H	O	92	89	205–208	212-213 [25]
8	4-Cl	OEt	H	S	88	80	208–210	176-177 [27]
9	3-Cl	OEt	H	O	74	72	185–187	190–192 [12]
10	2-Cl	OEt	H	O	78	77	190–192	220–222 [26]
11	2-Cl	OMe	H	O	80	82	245–248	252-253 [28]
12	3-OCH3	OEt	H	O	92	87	210–212	220-221 [29]
13	3-OCH3	OEt	H	S	88	84	214–216	—
14	2,4-Dimethyl	OEt	H	O	82	85	200–202	—
15	3,4-dimethyl	OEt	H	S	77	78	203–205	—
16	3-OH, 4-OCH3	OEt	H	O	84	81	225–227	230–232 [30]
17	3-OCH3, 4-OH	OEt	H	O	88	83	230–232	233–235 [30]
18	3,4,5- Trimethoxy	OEt	H	O	92	88	202–205	216–218 [24]
19	3,4,5- Trimethoxy	OMe	H	S	84	78	187–190	—
20	3,4,5- Trimethoxy	OMe	H	O	87	84	190–192	—
21	4-F	OEt	H	O	91	80	189–192	192–194 [24]
22	4-CF3	OEt	H	O	88	83	165–167	—
23	2-CF3	OEt	H	O	90	87	174–176	—
24	3-OH, 4-OCH3	CN	COCH3	S	89	88	210–212	—
25	3-OCH3, 4-OH	CN	COCH3	S	84	87	190–195	—
26	4-OH	CN	COCH3	S	92	88	186–190	—
27	4-Cl	CN	COCH3	S	90	87	196–198	—

^aThe reactions were carried out by grinding aromatic aldehyde (1.0 mmol), 1,3-dicarbonyl compounds (1.0 mmol), urea/thiourea/acetyl thiourea (2.0 mmol), and PPA or lithium-acetate (0.5 mmol) in mortar and pestle at room temperature for 5–10 minutes (Method II).