Raws li cov dej soluble raw khoom ntawm cov vitamins B, folic acidAPIyog synthesized los ntawm kev sib koom ua ke cov kev cai ntawm cov organic chemistry nrog kev sib npaug ntawm kev ua haujlwm lom neeg. Nws muaj cov yam ntxwv tshwj xeeb nrog rau kev ua haujlwm siab substrate, nruj stereochemical configuration tswj thiab ntau kauj ruam kev sib koom ua ke. Cov yam ntxwv no tsis tsuas yog lav qhov kev ua haujlwm lom neeg ntawm cov khoom lag luam tab sis kuj tseem ua kom muaj kev tsim khoom loj, muab cov ntaub ntawv zoo folic acid raw khoom rau kev lag luam kws tshuaj.
Qhov tshwj xeeb hauv kev xaiv cov khoom siv raw yog qhov tseem ceeb ntawm folic acid API synthesis. Nws cov synthesis siv p aminobenzoic acid, glutamic acid thiab pteridine derivatives ua cov ntaub ntawv tseem ceeb. Ntawm lawv, kev npaj ntawm lub nplhaib pteridine muaj ntau yam kev cuam tshuam cyclization, thiab raw khoom purity yuav tsum tshaj 99.9% los tiv thaiv impurities los ntawm kev cuam tshuam nrog cov condensation tom ntej.
P aminobenzoic acid yuav tsum muaj kev tiv thaiv acylation kom tsis txhob muaj kev cuam tshuam sab ntawm cov amino pawg nyob rau hauv qhov kub thiab txias. Xws li lub hom phiaj pretreatment ntawm raw cov ntaub ntawv nce cov txiaj ntsig ntawm cov ntsiab lus tseem ceeb mus rau ntau dua 85%, nteg lub hauv paus rau kev nce qib ntawm cov tshuaj tiv thaiv tom ntej. Qhov no txawv txawv ntawm cov khoom siv raw universality ntawm lwm cov vitamin APIs.
Kev tswj xyuas meej ntawm stereochemical configuration yog qhov kev sib tw tseem ceeb thiab qhov tshwj xeeb ntawm folic acid API synthesis. Cov folic acid molecule muaj ntau lub chaw chiral, nrog rau nws daim ntawv nquag ua haujlwm yog L configuration. Asymmetric catalysis technologies tau saws thaum lub sij hawm sib txuas los tswj kev teeb tsa, kom ntseeg tau qhov feem ntawm L isomers tshaj 99%. Nyob rau hauv cov kauj ruam condensation ntawm glutamic acid thiab pteroyl pawg, enzymatic catalysis hloov tshuaj synthesis. Glutamyl synthetase yog siv rau nws stereoselectivity, uas tsuas yog catalyzes cov tshuaj tiv thaiv ntawm L glutamic acid thiab pteroic acid kom tsis txhob tsim D configuration isomers. Kev sib xyaw ua ke ntawm biocatalysis thiab tshuaj synthesis txhim kho kev ua kom huv huv thiab txo cov nqi daws teeb meem, ua qhov tseem ceeb ntawm qhov txawv ntawm folic acid API los ntawm lwm cov vitamins achiral.
Kev sib koom tes optimization ntawm ntau kauj ruam cov tshuaj tiv thaiv qhia txog qhov tsis sib xws ntawm cov txheej txheem synthesis. Folic acid synthesis muaj ntau tshaj li rau qhov kev tshwm sim nrog rau pteridine nplhaib kev tsim kho, benzoylation thiab glutamic acid condensation, nrog rau cov xwm txheej zoo sib xws rau txhua kauj ruam. Pteridine nplhaib synthesis ua tiav nyob rau hauv tsis muaj zog alkaline tej yam kev mob (pH 8.0-8.5) ntawm 50-55℃los tiv thaiv lub nplhaib cleavage, thaum benzoylation tiav nyob rau hauv ib tug acidic ib puag ncig (pH 3.0-3.5) nrog cov tshuaj tiv thaiv tus nqi tswj los ntawm dropwise ntxiv ntawm acylating agents. Ib hom kev tsim khoom tas mus li tau txais los ntawm txhua kauj ruam, qhov twg cov neeg nruab nrab mus rau qib tom ntej yam tsis muaj kev lim dej. Qhov no nce tag nrho cov txiaj ntsig mus rau ntau dua 60%, nce 20% piv nrog cov khoom lag luam ib txwm muaj. Xws li ib qho kev sib koom ua ke zoo heev muab kev txhawb nqa tseem ceeb rau kev tsim khoom loj ntawm folic acid API.
Kev ua haujlwm khaws cia thev naus laus zis sawv cev rau qhov kev xav tau tshwj xeeb rau folic acid API synthesis. Lub nplhaib pteridine hauv folic acid yog rhiab rau lub teeb thiab kub. Tsawg kub crystallization (0-5 degree) hloov cov pa kub kub evaporation nyob rau tom qab synthesis theem kom tsis txhob degradation ntawm cov khoom xyaw nquag. Lub tshuab nqus tsev khov kom qhuav yog siv thaum ziab ntawm -40℃nrog lub tshuab nqus tsev kawm ntawv ntawm 0.01 Pa, tswj cov dej noo ntawm cov khoom tiav hauv qab 3% thaum khaws ntau dua 95% ntawm kev ua haujlwm lom neeg. Piv nrog rau cov vitamins ruaj khov xws li vitamin B1, folic acid API synthesis xav tau cov mob me me nyob rau theem kawg ntawm kev kho mob. Qhov kev tsom mus rau kev tuav haujlwm yog qhov tseem ceeb ntawm nws cov txheej txheem synthesis.
Cov khoom sib xyaw tshwj xeeb ntawm folic acid API qia los ntawm qhov nyuaj ntawm nws cov qauv molecular thiab rhiab heev ntawm nws txoj haujlwm lom neeg. Los ntawm kev xaiv cov khoom siv tshwj xeeb thiab kev tswj hwm kev tswj hwm tus kheej kom zoo rau kev sib koom ua ke ntawm ntau cov kauj ruam cov tshuaj tiv thaiv, ib qho kev sib npaug ntawm cov tshuaj lom neeg thiab kev ua haujlwm lom neeg tau tsim. Tsis zoo li cov txheej txheem hluavtaws yooj yim ntawm lwm cov vitamin APIs, kev sib sib zog nqus ntawm biocatalysis thiab tshuaj synthesis, nrog rau cov kev cai nruj rau kev tuav haujlwm, ua rau nws yog ib qho qauv ntawm cov vitamin synthesis. Nws muab cov txheej txheem xa mus rau kev tsim APIs nrog cov qauv nyuaj thiab cov kev xav tau ntawm kev ua haujlwm, qhia txog cov txiaj ntsig tseem ceeb ntawm cov thev naus laus zis zoo hauv kev ua kom muaj txiaj ntsig ntawm cov tshuaj.
