An efficient and safe process for the preparation of ticagrelor, a platelet aggregation inhibitor via resin-NO2 catalyzed formation of triazole ring

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Table 2 Optimization of mole ratio of compound 13 with respect to compound 14

Compd. 14 (g)	Compd. 13 (mol. eq)	Base	Catalyst	Temp (°C)	Reaction yield (%)	Isolated yield (%)	HPLC purity (%)
10.0	1.00	DIPEA	DBU	120–125	85.15	59.40	99.03
10.0	0.90	DIPEA	DBU	120–125	82.30	54.25	95.11
10.0	1.05	DIPEA	DBU	120–125	87.95	69.85	99.38
10.0	1.10	DIPEA	DBU	100–105	88.65	67.14	98.38
10.0	1.20	DIPEA	DBU	120–125	94.50	73.14	99.31
25.0	1.10	DIPEA	KI	120–125	91.85	73.00	99.51
10.0	1.10	DIPEA	–	120–125	89.45	67.97	99.60
10.0	1.10	DIPEA	DBU	135–140	92.20	72.00	99.30
100.0	1.10	DIPEA	DBU	120–125	94.90	79.95	99.37
100.0	1.10	DIPEA	DBU	120–125	95.05	80.81	99.35
100.0	1.10	DIPEA	DBU	120–125	94.65	79.96	99.57

All the reactions are performed in MEG. 10 volumes of MEG was used w. r. to compound 13 provided favourable results