Conditions for the synthesis of olanzapine derivatives in the reaction of DOLA (1 eq.) : 1–4 (1 eq.) : K₂CO₃ (3 eq.) : DABCO or TBAB (0.01 eq.) in MW or ultrasound.

EntryEE no.	Comp.	n	Conditions	Temp.a [°C]	Press.b [bar]	Solvent/base/catalyst	Reaction time [min]	Yield [%]
1	5	3	MW	150	2.8	DMF/K2CO3/DABCO	2	86
2	5	3	MW	150	0.3	NaDES/K2CO3/TBAB	2	30
3	5	3	MW	150	4.3	NaDES/Glycerine/K2CO3/TBAB	1.5	57
4	5	3	)))	45	Atm	DMF/K2CO3/TBAB	60	16
5	5	3	)))	45	Atm	DMF/K2CO3/TBAB	120	30
6	5	3	)))	45	Atm	H2O/K2CO3/TBAB	60	0
7	5	3	)))	45	Atm	H2O/K2CO3/TBAB	120	6
8	5	3	)))	45	Atm	H2O/K2CO3/DABCO	60	0
9	5	3	)))	65	Atm	H2O/K2CO3/DABCO	180	51
10	5	3	)))	45	Atm	NaDES/K2CO3/TBAB	120	1
11	5	3	)))	45	Atm	NaDES/K2CO3/TBAB	180	30
12	5	3	)))	45	Atm	NaDES/DIPEA/TBAB	120	10
13	6	4	MW	150	2.7	DMF/K2CO3/DABCO	2	65
14	6	4	MW	150	0.5	NaDES/K2CO3/TBAB	2	47
15	6	4	MW	150	1.5	NaDES/Glycerine/K2CO3/TBAB	3	40
16	6	4	)))	45	Atm	H2O/K2CO3/DABCO	120	1
17	6	4	)))	65	Atm	H2O/K2CO3/DABCO	180	0
18	6	4	)))	45	Atm	NaDES/K2CO3/TBAB	120	0
19	6	4	)))	45	Atm	NaDES/DIPEA/TBAB	120	10
20	7	5	MW	150	2.3	DMF/K2CO3/DABCO	2	57
21	7	5	MW	150	0.5	NaDES/K2CO3/TBAB	2	36
22	7	5	MW	150	4.2	NaDES/Glycerine/K2CO3/TBAB	2	13
23	7	5	)))	45	Atm	H2O/K2CO3/DABCO	120	7
24	7	5	)))	65	Atm	H2O/K2CO3/DABCO	180	27
25	7	5	)))	45	Atm	NaDES/K2CO3/TBAB	120	2
26	7	5	)))	45	Atm	NaDES/DIPEA/TBAB	120	0
27	8	6	MW	150	2.6	DMF/K2CO3/DABCO	2	70
28	8	6	MW	150	0.8	NaDES/K2CO3/TBAB	2	31
29	8	6	MW	150	2.8	NaDES/Glycerine/K2CO3/TBAB	3	5
30	8	6	)))	45	Atm	H2O/K2CO3/DABCO	120	0
31	8	6	)))	65	Atm	H2O/K2CO3/DABCO	180	31
32	8	6	)))	45	Atm	NaDES/K2CO3/TBAB	120	2
33	8	6	)))	45	Atm	NaDES/DIPEA/TBAB	120	0

^aHighest observed data entered; the maximum temperature was set to 150 °C; reactions in the presence of ultrasound were carried out under reflux.

^bHighest observed data entered; the maximum pressure was set to 10 bar.