Tong Q
PUMC Hospital, Beijing.
Zhongguo Yi Xue Ke Xue Yuan Xue Bao. 1990 Feb;12(1):42-5.
A new antihepatitic drug, BDD (I), which is very active and powerful especially in lowering elevated SGPT levels, has been previously discovered during the systematic study of Schisandra chinensis. In order to study the metabolism of this new antihepatic drug, deuterated BDD was prepared according to the following method. BDD lg, sodium chloroplatinate 193 mg, deuterium oxide 16ml, acetic anhydride 30ml, and acetyl chloride 0.4 ml were well mixed in a sealed ampoule and heated to 120-130 degrees C for 12h. The mixture was then poured into water. The precipitate (0.86g) contained the deuterated acid (IIa, IIb) of BDD. After esterification with methanol, a mixture (m.p. 150-153 degrees C) of mono- and di-deuterated BDD was obtained. Molecular clustering, as determined by GC/MS, showed that the product consisted of mono-deutero-BDD (IIIa) (m/e419) and dideutero-BDD (IIIb) (m/e420) in the ratio of 1:1.3.
一种新型抗肝炎药物BDD（I），尤其在降低升高的谷丙转氨酶水平方面具有很强的活性，此前在对五味子的系统研究中被发现。为了研究这种新型抗肝药物的代谢情况，按照以下方法制备了氘代BDD。将1克BDD、193毫克氯铂酸钠、16毫升重水、30毫升乙酸酐和0.4毫升乙酰氯在密封安瓿中充分混合，加热至120 - 130摄氏度12小时。然后将混合物倒入水中。沉淀物（0.86克）含有BDD的氘代酸（IIa，IIb）。用甲醇酯化后，得到单氘代和双氘代BDD的混合物（熔点150 - 153摄氏度）。通过气相色谱/质谱法测定的分子聚类表明，产物由单氘代BDD（IIIa）（m/e419）和双氘代BDD（IIIb）（m/e420）组成，比例为1:1.3。
