长效口服避孕药复方炔雌醚已在临床使用

[1]

，为了进一步研究其代谢规律，我们拟采用放射免疫法测定血液中炔雌醚浓度。高比度甾体雌激素氚标记化合物的制备一般采用C-6

7或C-2

4

6

7位氚标记，可是雌激素在体内要代谢为6α-羟和6-酮等代谢产物，所以它们用于代谢研究会造成误差

[2]

。为使氚标记物既能用于放射免疫测定，又可用于代谢分布和作用机制的研究，我们选择了C-9

11位氚标记炔雌醚

[3

4]

，合成反应式为：

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The preparation of [9

11-

3

H]-quinestrol is reported. Estrone 3-cyclopentyl ether

was first oxidized by 2

3-dichloro-5

6-dicyano-quinone (DDQ) to get the dehydrogenated precursor at 9

11-positions. This was tritiated with 5% palladium-carbon catalyst to produce [9

11-

3

H]-estrone 3-cyclopentyl ether

then turned to [9

11-

3

H]-quinestrol by ethynylation with acetylene-butyllithium. The final product had a specific activity of 26 Ci/m

M

.