Preparation method of meto-Iodobenzylguanidine

Abstract

The invention relates to a preparation method of <131>I-MIBG (meto-Iodobenzylguanidine). The method comprises the following steps: heating meto-Iodobenzylguanidine sulfate, stannous mono-sulphate, a reducing agent, copper sulfate and Na<131>I in a boiling water bath, standing after finishing the reaction, taking a supernatant liquid, and filtering the supernatant liquid with a microfiltration membrane. Sodium thiosulfate and / or sodium thiosulfate are / is taken as the reducing agent to prepare the meto-Iodobenzylguanidine sulfate, the prepared <131>I-MIBG is high in radiochemical purity and good in stability, and the radiochemical purity of the prepared <131>I-MIBG is still at a relatively high level after 48 hours.

Description

technical field

[0001] The invention relates to the field of radiopharmaceuticals, in particular to a preparation method of m-iodobenzylguanidine. Background technique

[0002] Pheochromocytoma located in the adrenal gland is a hormone-secreting tumor with adrenal medulla function, and in hypertensive patients, 0.6%-1.0% are caused by pheochromocytoma. Patients may be life-threatening due to severe heart, brain, and kidney damage caused by long-term hypertension or sudden severe secondary hypertension. Adrenal medullary lesions mainly include: pheochromocytoma and medullary hyperplasia, which are mainly manifested clinically as paroxysmal or persistent hypertension. Different from essential hypertension, the hypertension caused by adrenal medulla lesions can return to normal in most patients as long as the lesion is surgically removed. Therefore, early diagnosis and treatment can cure this secondary disease. High blood pressure.

[0003] Inter-iodobenzylguanidine (metaiod...

Examples

preparation example Construction

[0032] 4) Preparation of m-iodobenzylguanidine sulfate (D)

[0033] Weigh 539mg (1.6mmol) of (C) and suspend it in 5mL of water, add 0.8mL (1.6mmol) of 2mol / L sulfuric acid dropwise, heat to dissolve it all, cool to room temperature, a white solid precipitates, filter with suction to obtain 515mg, and use ethanol for the solid Recrystallized with water to obtain 472mg, yield 91.2%, m.p166-167℃.

[0034] 2. Preparation of labeled m-iodobenzylguanidine sulfate 131 I-MIBG

Embodiment 1

[0035] Embodiment 1: Add m-iodobenzylguanidine sulfate 1mg successively in glass test tube, stannous sulfate 0.5mg, sodium thiosulfate 0.1mmol, copper sulfate 0.43mg and radioactivity are the Na of 5mCi 131 I solution, put it in a boiling water bath and heat for 30 minutes, take it out, put it in a beaker, let it stand for 30 seconds, absorb the supernatant, and pass it through a 0.22μm filter membrane to obtain the marker 131 I-MIBG.

Embodiment 2

[0036] Embodiment 2: Add m-iodobenzylguanidine sulfate 1mg successively in glass test tube, stannous sulfate 0.5mg, sodium sulfite 0.1mmol, copper sulfate 0.43mg and radioactivity are the Na of 5mCi 131 I solution, put it in a boiling water bath and heat for 30 minutes, take it out, put it in a beaker, let it stand for 30 seconds, absorb the supernatant, and pass it through a 0.22μm filter membrane to obtain the marker 131 I-MIBG.

technical field

[0001] The invention relates to the field of radiopharmaceuticals, in particular to a preparation method of m-iodobenzylguanidine. Background technique

[0002] Pheochromocytoma located in the adrenal gland is a hormone-secreting tumor with adrenal medulla function, and in hypertensive patients, 0.6%-1.0% are caused by pheochromocytoma. Patients may be life-threatening due to severe heart, brain, and kidney damage caused by long-term hypertension or sudden severe secondary hypertension. Adrenal medullary lesions mainly include: pheochromocytoma and medullary hyperplasia, which are mainly manifested clinically as paroxysmal or persistent hypertension. Different from essential hypertension, the hypertension caused by adrenal medulla lesions can return to normal in most patients as long as the lesion is surgically removed. Therefore, early diagnosis and treatment can cure this secondary disease. High blood pressure.

[0003] Inter-iodobenzylguanidine (metaiod...

Examples

preparation example Construction

[0032] 4) Preparation of m-iodobenzylguanidine sulfate (D)

[0033] Weigh 539mg (1.6mmol) of (C) and suspend it in 5mL of water, add 0.8mL (1.6mmol) of 2mol / L sulfuric acid dropwise, heat to dissolve it all, cool to room temperature, a white solid precipitates, filter with suction to obtain 515mg, and use ethanol for the solid Recrystallized with water to obtain 472mg, yield 91.2%, m.p166-167℃.

[0034] 2. Preparation of labeled m-iodobenzylguanidine sulfate 131 I-MIBG

Embodiment 1

[0035] Embodiment 1: Add m-iodobenzylguanidine sulfate 1mg successively in glass test tube, stannous sulfate 0.5mg, sodium thiosulfate 0.1mmol, copper sulfate 0.43mg and radioactivity are the Na of 5mCi 131 I solution, put it in a boiling water bath and heat for 30 minutes, take it out, put it in a beaker, let it stand for 30 seconds, absorb the supernatant, and pass it through a 0.22μm filter membrane to obtain the marker 131 I-MIBG.

Embodiment 2

[0036] Embodiment 2: Add m-iodobenzylguanidine sulfate 1mg successively in glass test tube, stannous sulfate 0.5mg, sodium sulfite 0.1mmol, copper sulfate 0.43mg and radioactivity are the Na of 5mCi 131 I solution, put it in a boiling water bath and heat for 30 minutes, take it out, put it in a beaker, let it stand for 30 seconds, absorb the supernatant, and pass it through a 0.22μm filter membrane to obtain the marker 131 I-MIBG.