The Synthesis Of Hydralazine Hydrochloride, Lamivudine And N-ethyl-L-menthylformylamine

This paper is maked up of the synthesis of hydralazine hydrochloride, Lamivudine and N-ethyl-L-menthylformylamine.The first part is on the synthesis of hydralazine hydrochloride,whose chemical name is 1-(phthalazin-1-yl)hydrazine hydrochloride.It is a kind of the active remedy that is a antihypertensive drugs.It was selled in the drugstore a long time ago.But it was due of its badly side effect,so that it was eliminated gradually.In 2006,a medicine study found that hydralazine hydrochloride used with isosorbide mononitrate can hold its effect and remove side effect.So it is used again.And hydralazine hydrochloride is a material.The paper introduces hydralazine hydrochloride simply.Through trying different reaction conditions,we founed a better routes,which can get a high yield and a lowest cost.This process route which needs simple raw materials is easy to industrial production.The structure of products was verificated by ¹HNMR,and IR.The second part is on the synthesis of Lamivudine,its chemical name is 2-deoxy-3-thiacytidine(2R-cis)-4-Amino-1-[2-(hydroxymethyl)-1,3-oxathiolan-5-yl]-2(1H)-pyrimidinone.It is a new kind of anti-HIV agent from nucleoside,which is produced by the Biochem Pharma Company in Canada.It may be useful in treatment of all kinds of hepatitis B.Its chemical properites,pharmacokinetic feature, mechanism of action,clinical uses,adverse drug reactions,and drug resistance are reviewed.We have compared about many synthesis routes of Lamivudine and have explored a new route to approach the terminate,which is (2R,5R)-((1R,2S,5R)-2-isopropyl-5-methylcyclohexyl) 5-hydroxy-1,3-oxathiolane-2-carboxylate as material.Through chlorination,coupling, hydrolyze and anhydrous reduction,we get the end production Lamivudine.We take benzaldehyde to protect cytosine,so that cut down dosage of hexamethyldisilazane and affect of hexamethyldisilazane.At the same time improve the route and slove the problem retrieve of slovent.The route is a beteer synthesie of Lamivudine.The structure of end production was verificated by ¹HNMR,¹³CNMR and MS.The third part is on the synthesis of.The cooling agent WS-3.The chemical name is N-ethyl-L-menthylformylamine.WS-3(N-ethyl-L-menthylformylamine) is a cooling agent,its cooling effect is very especial,so people pay more attention to it.The paper have compared about some sythesies of WS-3,we improve the synthesis.The ws-3 was prepared from(1R,2S,5R)-(-)-menthol as starting material, through chlorination with triphosgene,cyanidation with sodium cyanide,hydrolyze, and amidization in the DCC four steps.We could get the end production.