3-Amino-4-pyrazole carbosamide hemisulfate

Agbedemeji fun iṣelọpọ ti allopurinol.

O jẹ ọkan ninu 3-amino-4-fidipo pyrazole jara.O le ṣee lo bi agbedemeji lati ṣajọpọ ọpọlọpọ awọn agbo ogun elegbogi ti o munadoko ti oogun, gẹgẹ bi allopurinol, ọkan ninu jara awọn itọsẹ pyrazolopyrimidine, igbehin lati ọdun 1963 Lati lilo ile-iwosan rẹ, o ti jẹ oogun akọkọ fun itọju gout.Lọwọlọwọ, awọn ọna ti a mọ diẹ wa fun sisọpọ

3-aminopyrazole-4-carboxamide hemisulfate ni Ilu China, nipataki nipa didaṣe malononitrile ati triethyl orthoformate lati mura ethoxymethylene malononitrile, ati lẹhinna pẹlu iṣesi ti hydrazine hydrate ti n pese 3-amino-4-cyanopyrazole, eyiti a ṣe nikẹhin pẹlu iṣelọpọ sulfuric acid.

3-aminopyrazole-4-carboxamide hemisulfate (Chen Huiru, Xiao Guomin et al. 3-aminopyrazole- Synthesis of 4-formamide hemisulfate [J]. Chemical Industry Times, 2008, 6 (22): 39 40), lapapọ ikore ti synthesis nipasẹ ọna yii jẹ nipa 60% (ti a ṣe iṣiro bi malononitrile), ọna yii O jẹ iṣesi-igbesẹ mẹta, awọn igbesẹ ti gun, ati awọn reagents ti a lo, gẹgẹbi malononitrile ati ethoxymethylene malononitrile, jẹ majele ati gbowolori.Ni afikun, 3-aminopyrazole-4 ti a pese sile nipasẹ ọna yii -Formamide hemisulfate ni awọ ti o ṣoro lati yọ kuro ati pe o nilo afikun sisẹ, eyiti o jẹ idiju diẹ sii.

Awọn ijabọ wa ni awọn iwe ajeji ti o nlo pyridylamide hydrazone ati ethoxymethylene malononitrile gẹgẹbi awọn ohun elo aise lati gba 3-amino-4-cyanopyrazole nipasẹ afikun ati cyclization, ati lẹhinna fesi pẹlu sulfuric acid ti o ni idojukọ lati gba ibi-afẹde afojusun (Reuken G Jones. Awọn aati ti orthoesters pẹlu awọn agbo ogun ti nṣiṣe lọwọ [J]. J Am Chem Soc. 1952,74 (5): 4889 4891).Awọn ohun elo aise akọkọ ti a lo ni ọna yii jẹ gbowolori, ikore esi ko ga, ati èrè ti iṣelọpọ ile-iṣẹ jẹ kekere.O gbodo soro.