Octreotide acetate hmoovyog ib qho kev sib xyaw ua ke ntawm somatostatin. Nws yog ib qho octapeptide compound uas muaj cov amino acids txuas nrog peptide bonds. Nws cov mis molecular yog C53H74N10O13S2 • C2H4O2, CAS 83150-76-9, nrog ib tug txheeb ze molecular luj ntawm 1129.38. Vim muaj ntau yam peptide thiab thioether daim ntawv cog lus hauv nws cov qauv, nws cov khoom siv tshuaj lom neeg kuj ruaj khov thiab nws muaj qee qhov ua rau lub teeb, kub, thiab acidity. Nws yog cov kua uas tsis muaj xim los yog yuav luag tsis muaj xim tsis muaj xim vim nws cov solubility siab nyob rau hauv aqueous daws thiab cov tshuaj ruaj khov. Lub solubility hauv dej yog qhov siab, tab sis nws kuj yog yooj yim soluble nyob rau hauv feem ntau siv organic solvents xws li ethanol thiab acetone. Qhov no zoo heev solubility tso cai rau Octreotide acetate tau yooj yim tov nrog lwm yam tshuaj los yog kuab tshuaj. Cov khoom siv tshuaj lom neeg muaj kev ruaj khov, tab sis nyob rau hauv cov xwm txheej hnyav xws li kub siab, muaj zog acid lossis lub hauv paus muaj zog, decomposition lossis polymerization tshwm sim tuaj yeem tshwm sim. Lub viscosity cuam tshuam los ntawm qhov kub thiab txias. Ntawm qhov kub thiab txias, nws viscosity yuav nce; Nyob rau hauv qhov kub thiab txias, nws viscosity yuav txo.
(Cov khoom txuas: https://www.bloomtechz.com/synthetic-chemical/api-researching-only/octreotide-acetate-powder-cas-83150-76-9.html)
Txoj Kev 1:
Cov kauj ruam ntxaws ntxaws rau kev tsim cov phosphatidylethanolamine (cephalin) siv cov diglycerides thiab txuas phospholipids nrog polyethylene glycol monomethyl ether los ntawm amide thiab ester bonds siv binary anhydride yog raws li hauv qab no:
1. Cov synthesis ntawm diglycerides: Triglycerides yog synthesized los ntawm esterification ntawm glycerol thiab fatty acids. Txoj kev sib xyaw tshwj xeeb yog kom sov glycerol thiab fatty acids nyob rau hauv qhov kev txiav txim ntawm acidic catalyst, ua rau glycerol thiab fatty acids mus rau esterification cov tshuaj tiv thaiv, tsim cov diglycerides. Qhov kev sib npaug tshuaj lom neeg tshwj xeeb yog raws li hauv qab no:
RCOH + HOCH2CH (OH) CH2OH → ROOCH2CH (OH) CH2OOCCH2CH3 + H2O
Ntawm lawv, RCOOH sawv cev rau fatty acids, thiab HOCH2CH (OH) CH2OH sawv cev rau glycerol.
2. Synthesis ntawm phosphatidylethanolamine: Reacting diglycerides nrog ethanolamine los tsim phosphatidylethanolamine. Qhov kev sib npaug tshuaj lom neeg tshwj xeeb yog raws li hauv qab no:
RCOOCH2CH (OH) CH2OOCCH2CH3+ NH3→ ROV2CH (OH) CH2OOCCH2CH2CH2NHCH2CH2OH
Ntawm lawv, RCOOCH2CH (OH) CH2OOCCH2CH3 sawv cev rau diglycerides, thiab NH3 sawv cev rau ethanolamine.
3. Lub synthesis ntawm polyethylene glycol monomethyl ether: polyethylene glycol reacts nrog formaldehyde los tsim polyethylene glycol monomethyl ether. Qhov kev sib npaug tshuaj lom neeg tshwj xeeb yog raws li hauv qab no:
NHOCH2CH2OCH2CH2OH + nHCHO → HOCH2CH (UA2CH2) nCH3+ nH2O
Ntawm lawv, HOCH2CH2OCH2CH2OH sawv cev rau polyethylene glycol, thiab HCHO sawv cev rau formaldehyde.
4. Synthesis ntawm Osteotide acetate: Phosphatidyl ethanolamine reacted nrog polyethylene glycol monomethyl ether los tsim Osteotide acetate. Qhov kev sib npaug tshuaj lom neeg tshwj xeeb yog raws li hauv qab no:
RCOOCH2CH (OH) CH2OOCCH2CH2CH2NHCH2CH2OH + HOCH2CH (UA2CH2) nCH3→ ROV2CH (UA2CH2) nNHCO-PEG-C49H66N10O10S2
RCOOCH2CH (OH) CH2OOCCH2CH2CH2NHCH2CH2OH sawv cev rau phosphatidylethanolamine, thiab HOCH2CH (OCH2CH2) nCH3 sawv cev rau polyethylene glycol monomethyl ether.
Txoj Kev 2:
Cov kauj ruam ntxaws ntxaws rau kev sib txuas ntawm PEG muab tau los ntawm phospholipids los ntawm kev sib txuas ncaj qha glycerol diesters nrog polyethylene glycol monomethyl ether siv phosphorus oxychloride yog raws li hauv qab no:
1. Npaj diglycerides thiab polyethylene glycol monomethyl ether: Dissolve diglycerides thiab polyethylene glycol monomethyl ether cais hauv cov kuab tshuaj organic xws li chloroform lossis methanol. Cov concentrations ntawm diglycerides thiab polyethylene glycol monomethyl ether tuaj yeem hloov kho raws li kev sim.
2. Ntxiv phosphorus oxychloride: Maj mam ntxiv cov dej sib tov ntawm diglycerides thiab polyethylene glycol monomethyl ether rau phosphorus oxychloride thiab do tsis tu ncua. Phosphorus oxychloride ua hauj lwm raws li phosphorylation reagent nyob rau hauv cov tshuaj tiv thaiv no, txuas diglycerides nrog polyethylene glycol monomethyl ether.
3. Cov txheej txheem tshuaj tiv thaiv: Ua cov tshuaj tiv thaiv ntawm chav tsev kub thiab ua kom nplawm. Thaum cov txheej txheem tshuaj tiv thaiv, nws tuaj yeem pom tias cov xim sib tov maj mam hloov, uas yog vim muaj cov tshuaj tiv thaiv ntawm phosphorus oxychloride nrog diglycerides thiab polyethylene glycol monomethyl ether.
4. Kev tshem tawm cov tshuaj tiv thaiv: Thaum cov tshuaj tiv thaiv mus txog lub sijhawm xav tau, cov tshuaj tiv thaiv tuaj yeem raug txiav los ntawm kev ntxiv cov dej uas tsim nyog. Ntxiv dej tuaj yeem hnov mob nrog phosphorus oxychloride los tsim phosphoric acid thiab hydrogen chloride, yog li txwv tsis pub cov tshuaj tiv thaiv.
5. Kev sib cais thiab kev ua kom huv: Ncuav cov tshuaj tiv thaiv rau hauv qhov sib cais, ntxiv cov dej uas tsim nyog rau kev ntxuav kom tshem tawm cov phosphorus oxychloride ntau dhau, cov diglycerides uas tsis muaj kev cuam tshuam, thiab polyethylene glycol monomethyl ether. Tom qab ntawd, cov khoom tau tuaj yeem raug ntxuav los ntawm txoj kev xws li recrystallization thiab chromatography los txhim kho nws cov purity thiab crystallinity.
6. Kev kuaj xyuas thiab kev txheeb xyuas: Cov yam ntxwv ntawm cov khoom tau txais Octreotide acetate tau ua los ntawm kev siv spectroscopic xws li nuclear magnetic resonance hydrogen spectroscopy thiab mass spectrometry kom paub meej tias nws cov qauv zoo li qhov kev cia siab. Nyob rau tib lub sijhawm, kev ntsuam xyuas zoo ntawm cov tau txais Octreotide acetate kuj tseem tuaj yeem ua los ntawm cov txheej txheem xws li kev txiav txim siab melting point thiab cov ntsiab lus tsom xam kom ntseeg tau tias nws qhov zoo thiab purity ua tau raws li qhov yuav tsum tau ua.
Qhov sib npaug tshuaj sib npaug yog:
RCOOCH2CH (OH) CH2OCCH2CH3+ P (OCl)3→ ROV2CH (UA2CH2) nCH3+ PIB2H + HCl
POCl2H + H2O → H3PO3+ HCl
Ntawm lawv, RCOOCH2CH (OH) CH2OOCH2CH3 sawv cev rau triglycerides, P (OCl) 3 sawv cev rau phosphorus oxychloride, POCl2H sawv cev rau dihydrogen phosphite, thiab H3PO3 sawv cev phosphoric acid.
Tsis tas li ntawd, cov teeb meem kev nyab xeeb yuav tsum tau muab rau hauv kev txiav txim siab thaum tsim cov Octreotide acetate hauv chav kuaj. Piv txwv li, thaum siv acidic catalysts thiab organic solvents, yuav tsum tau them nyiaj mloog mus rau tiv thaiv acid thiab hnyav tshuaj lom; Thaum siv hluav taws xob hluav taws xob siab thiab lub zog hluav taws xob lasers, kev tswj xyuas kev nyab xeeb yuav tsum ua raws li; Thaum siv cov tshuaj tsis zoo uas feem ntau siv rau hauv cov organic synthesis, yuav tsum tau them nyiaj rau kev hnav cov cuab yeej tiv thaiv tus kheej thiab ua raws li cov cai hauv kev nyab xeeb. Nyob rau tib lub sijhawm, txhawm rau tiv thaiv ib puag ncig, nws yog ib qho tsim nyog yuav tsum tau ua thiab pov tseg cov khoom pov tseg uas tsim tawm thiab pov tseg kom tsim nyog.