EJNMMI Radiopharmacy and Chemistry

Table 1 Effect of the solvent and temperature on the RCY of [¹¹C]7m6BP

From: Improved synthesis of 6-bromo-7-[¹¹C]methylpurine for clinical use


Entry	Solvent	T (°C)	[¹¹C]CH₃I^b	RCY (%)^a		Ratio^c
Entry	Solvent	T (°C)	[¹¹C]CH₃I^b	[¹¹C]7m6BP	[¹¹C]9m6BP	Ratio^c
1	ACT	100	0.067	24	52	0.46
2	MeCN	100	0.036	25	51	0.49
3	DMF	100	0	26	65	0.40
4	AcOMe	100	49	24	21	1.1
5	AcOMe	140	7.5	41	39	1.1
6	AcOMe	180	0.036^d	38	38	1.0
7	AcOEt	100	58	20	16	1.2
8	AcOEt	140	25	33	30	1.1
9	AcOEt	180	4.8	39	37	1.1
10	MP	100	76	12	9.4	1.3
11	MP	140	29	34	28	1.2
12	MP	180	6.8	42	35	1.2
13	THF	100	32	34	28	1.2
14	THF	140	6.6	45	38	1.2
15	THF	180	0.97	43	36	1.2
16	1,3-DO	100	7.4	35	43	0.82
17	1,3-DO	140	1.1	37	48	0.77
18	1,3-DO	180	0.14	30	38	0.78
19	2-MeTHF	100	92	4.1	2.2	1.9
20	2-MeTHF	140	80	12	6.0	2.0
21	2-MeTHF	180	61	19	10	1.9
22	1,4-DO	100	92	3.3	1.7	1.9
23	1,4-DO	140	81	9.3	4.7	2.0
24	1,4-DO	180	57	19	10	1.9
25	iPr₂O	100	98	Trace	Trace	–
26	iPr₂O	140	96	Trace	Trace	–
27	iPr₂O	180	94	Trace	Trace	–
28	CHCl₃	100	95	Trace	Trace	–
29	CHCl₃	140	94	Trace	Trace	–
30	CHCl₃	180	94	Trace	Trace	–
31	Tol	100	96	Trace	Trace	–
32	Tol	140	96	Trace	Trace	–
33	Tol	180	94	Trace	Trace	–
34	DCM	100	98	Trace	Trace	–

[¹¹C]7m6BP was manually synthesized using [¹¹C]CH₃I (n = 1)
^aDetermined by radio-HPLC and TLC analysis of the crude product
^bUnreacted [¹¹C]CH₃I
^cRatio of [¹¹C]7m6BP/[¹¹C]9m6BP
^dAcOMe in the vial sealed with a screw cap was evaporated under these conditions, and thus the calculation of the proportion of unreacted [¹¹C]CH₃I was not reliable

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