| 摘要 |
The invention relates to a process for preparation of a compound of formula (I):;R1 is selected from C1-6alkyl, C2-6alkenyl, and C2-6alkynyl;which comprises:(i) reaction with fluoride, suitably [18F]fluoride, of a corresponding compound of formula (II):;wherein R2 is selected from hydrogen, C1-10alkyl, C1-10haloalkyl, C6-14aryl, C6-14arylalkyl, —(CH2CH2O)q—CH3 wherein q is an integer of from 1 to 10;R1 is as defined for the compound of formula (I); andR3 is a leaving group. Certain novel precursors of formula (II) and radiopharmaceutical kits containing such precursors are also claimed. |
| 主权项 |
1. A compound of formula (IIa),wherein
R1 is C1-6alkyl, C2-6alkenyl, or C2-6alkynyl; phenyl ring A is substituted by 1 to 3 substituents being chosen from any of the non-phenyl substituents defined for R7 to R10; R2 is hydrogen, C1-10alkyl, C1-10haloalkyl, C6-14aryl, C6-14arylalkyl, or —(CH2CH2O)q—CH3 where q is an integer of from 1 to 10; R3 is nitro, —N2+, chloro, bromo, iodo, —NR4(C1-6alkyl)2+ where R4 is C1-6alkyl, —OSO2R5where R5 is C1-6alkyl, C1-6haloalkyl, or aryl, or where R6 is hydrogen, C1-6alkyl, halo, aor nitro;
R7, R8, R9, and R10 are each independently, fluoro, chloro, bromo, iodo, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, (CH2)mOR11 (where m is 1, 2, or 3), CF3, CH2—CH2Y, O—CH2—CH2Y, CH2—CH2—CH2Y, O—CH2—CH2—CH2Y (where Y is fluoro, chloro, bromo, or iodo), CN, (C═O)—R11, N(R11)2, NO2, (C═O)N(R11)2, O(CO) R11, OR11, SR11, COOR11, Rph, CR11═CR11—Rph, CR112—CR112—Rph (where Rph is an unsubstituted or substituted phenyl group with the phenyl substituents being chosen from any of the non-phenyl substituents defined for R7 to R10 and where R11 is H or C1-6alkyl) or a protected derivative of any thereof. |
