Phenobarbital(Benzobarbital) yog ib qho tshuaj, dawb los yog dawb siv lead ua hmoov, yooj yim soluble hauv chloroform, ethanol thiab ether, me ntsis soluble hauv dej.
Txoj kev hluavtaws ntawm phenobarbital feem ntau suav nrog cov kauj ruam hauv qab no:
1. Synthesis ntawm methyl phenylacetate: benzoic acid thiab formic acid yog condensed thiab dehydrated los tsim methyl phenylacetate.
2. Synthesis ntawm phenylacetyl chloride: methyl phenylacetate reacts nrog thionyl chloride los tsim phenylacetyl chloride.
3. Synthesis of phenobarbital precursor-5-phenyl-5-isovaleric acid (5-Phenyl-5-isopropylbarbituric acid): phenylacetyl chloride reacts nrog isovaleryl urea los tsim 5-phenyl{ {6}} Isovaleric acid.
4. Synthesis of phenobarbital: react 5-phenyl-5-isovaleric acid thiab ethanolamine nyob rau hauv alkaline tej yam kev mob los tsim phenobarbital.
Txoj kev ua tiav hluavtaws ntawm phenobarbital yog raws li hauv qab no:
Benzoic acid ntxiv rau formic acid → methyl phenylacetate
Tom ntej: Methyl phenylacetate plus thionyl chloride → phenylacetyl chloride
Phenylacetyl chloride ntxiv isovaleryl urea → 5-phenyl-5- isovaleric acid
5-Phenyl-5-isovaleric acid ntxiv rau ethanolamine → phenobarbital
Nws yuav tsum raug sau tseg tias qhov no tsuas yog ib txoj hauv kev rau kev sib txuas ntawm phenobarbital, thiab cov txheej txheem synthesis tiag tiag yuav txawv me ntsis vim qhov kev npaj sib txawv. Thaum ua haujlwm hauv chav kuaj, kev nyab xeeb yuav tsum tau them rau, thiab kev ua haujlwm tsim nyog thiab xaiv cov khoom siv yuav tsum tau ua raws li qhov xwm txheej tiag tiag.
Benzobarbital laboratory synthesis method cov kauj ruam yog raws li nram no:
1. Synthesis ntawm methyl phenylacetate:
Nyob rau hauv sib nqus stirring, sib tov benzoic acid thiab formic acid thiab maj mam ntxiv sulfuric acid catalyst (1 mL). Rhaub rau 80 degree thiab reacted rau 4 teev. Tom qab txias, ntxiv 10 feem pua sodium hydroxide tov los kho cov pH rau 8-9. Cov khoom tau muab rho tawm 3 zaug nrog ether kom tau methyl phenylacetate.
2. Synthesis ntawm phenylacetyl chloride:
Hauv ib lub raj xa dej, sib tov methyl phenylacetate thiab thionyl chloride, thiab ntxiv me me ntawm catalyst (concentrated sulfuric acid). Tom qab nplawm rau 1 teev, cov precipitate raug tshem tawm los ntawm kev pom kom tau phenylacetyl chloride.
3. Synthesis ntawm 5-phenyl-5-isovaleric acid:
Hauv ib lub raj xa dej, sib tov phenylacetyl chloride thiab isovaleryl urea, thiab ntxiv sodium carbonate catalyst. Rhaub kom reflux thiab nplawm rau 2 teev kom tau txais 5-phenyl-5-isovaleric acid.
4. Synthesis ntawm phenobarbital:
Sib tov 5-phenyl-5-isovaleric acid thiab ethanolamine, ntxiv ib qho me me ntawm sodium hydroxide tov rau cov khoom siv reflux, thiab cua sov rau reflux rau 1 teev. Tom qab txias, kua qaub tau ntxiv los kho cov pH rau acidic, cov khoom tau muab rho tawm peb zaug nrog chloroform, thiab cov khoom tau sau los ntawm distillation kom tau txais phenobarbital crystals.
Nws yog ib qho tseem ceeb uas yuav tsum nco ntsoov tias phenobarbital yog ib qho tshuaj narcotic thiab tsuas yog yuav tsum tau muab coj los siv hauv chav kuaj mob. Kev nyab xeeb yuav tsum tau them sai sai rau thaum lub sijhawm sim, thiab kev ua haujlwm yuav tsum tau ua raws li cov txheej txheem kev sim thiab kev nyab xeeb ntawm kev ua haujlwm.
Phenobarbital (Benzobarbital) yog ib qho barbiturate uas tau tsim thawj zaug hauv xyoo 1902 los ntawm Fab Kis kws tshuaj Eugene Schloesing.
Nrog rau cov synthesis ntawm phenobarbital, tib neeg pib kawm nws cov tshuaj pharmacological, thiab pom tias nws muaj hypnotic, anxiolytic thiab antiepileptic teebmeem. Yog li ntawd, phenobarbital tsis ntev tau siv nyob rau hauv kev kho mob teb thiab tau los ua ib tug nquag siv sedative, hypnotic thiab antiepileptic tshuaj.
Nyob rau hauv lub xyoo pua 20th, kev siv phenobarbital muaj ntau heev, tab sis raws li nws cov kev mob tshwm sim tau nkag siab zoo dua, nws siv tau maj mam txwv. Hauv xyoo 1950, kev siv phenobarbital maj mam txo qis nrog kev qhia txog benzodiazepines (phenobarbital analogs).
Txawm hais tias kev siv phenobarbital tsuas yog txwv, nws tseem ua lub luag haujlwm hauv kev tshawb fawb kho mob, xws li inducer hauv kev sim tsiaj. Tsis tas li ntawd, txoj kev tshawb fawb ntawm phenobarbital tseem yuav pab peb nkag siab zoo txog cov tshuaj pharmacological ntawm cov tshuaj sedatives thiab hypnotics, thiab txhawb kev tshawb fawb thiab kev loj hlob ntawm cov tshuaj muaj feem xyuam.
Txawm hais tias phenobarbital tau siv dav hauv yav dhau los, nws siv tsis tshua muaj hnub no. Qhov no yog vim tias phenobarbital muaj cov kev mob tshwm sim loj xws li kev vam khom, tshuaj tiv thaiv, kev siv tshuaj ntau dhau tuaj yeem ua rau ua pa tsis ua haujlwm, thiab lwm yam, thiab muaj kev nyab xeeb thiab siv tau zoo dua lwm yam tshuaj muaj.
Yog li ntawd, los ntawm kev xav ntawm kev kho mob daim ntawv thov, lub zeem muag ntawm phenobarbital yog tsis optimistic. Txawm li cas los xij, los ntawm qhov kev xav ntawm kev tshawb fawb tshuaj thiab kev loj hlob, phenobarbital tseem muaj qee yam peev xwm. Phenobarbital tuaj yeem siv los ua ib qho kev siv rau kev kawm ntawm lwm cov barbiturates los pab kom nkag siab zoo txog cov tshuaj ntawm cov tshuaj no. Tsis tas li ntawd, cov qauv ntawm phenobarbital tuaj yeem siv los tsim cov tshuaj tshiab molecules los txhim kho qhov tsis zoo thiab qhov tsis zoo ntawm barbiturates.
Feem ntau hais lus, txawm hais tias daim ntawv thov kev kho mob qhov kev cia siab ntawm phenobarbital tsis zoo, nws tseem muaj qee yam peev xwm hauv kev tshawb fawb tshuaj thiab kev loj hlob.