Clascoteroneyog ib hom tshuaj kho pob txuv tshiab uas tau nyiam ntau yam vim nws cov txiaj ntsig zoo. Nws lub npe tshuaj yog 17-hydroxy-6,9,11,13 -tetramethyl-1,2,6,7,8,9,10,11,12,13, 14,15,16,17-tetradecahydrocyclopenta[a] Phenanthren-3-ib tug, uas nws cov tshuaj formula yog C24H34O2, muaj ib tug hnyav molecular ntawm 354.52. Nws yog dawb los yog tawm-dawb siv lead ua los yog crystalline hmoov. Nws yooj yim soluble hauv dichloromethane, yooj yim soluble hauv methanol, thiab insoluble hauv dej. Nws yog siv rau hauv kev tshawb fawb thiab tshuaj reagents, organic synthesis, thiab tshuaj intermediates.
Txoj kev synthesis thiab cov kauj ruam ntxaws ntxaws ntawm Clascoterone feem ntau yog qhia.
Synthetic txoj kev:
1. Pib los ntawm 7-methyl-2-oxo-1,2,3,4-tetrahydronaphthalene, ua tsib alkylation cov tshuaj tiv thaiv kom tau txais 17-methyl{{8} }ethyl-2-oxo -1,2,3,{13}}tetrahydronaphthalene.
2. Hydroxylation ntawm 17-methyl-7-ethyl-2-oxo-1,2,3,4-tetrahydronaphthalene kom tau txais 17-hydroxy{{9} }ethyl{10}}oxo-1 ,2,3,{14}}Tetralin.
3. Oxidation ntawm 17-hydroxy-7-ethyl-2-oxo-1,2,3,4-tetralin kom tau txais 17-formyl{{9} }ethyl-2-oxo-1, 2,3,{14}}tetrahydronaphthalene.
4. Txo ntawm 17-formyl-7-ethyl-2-oxo-1,2,3,4-tetrahydronaphthalene los ntawm carbonyl kom tau txais 17-hydroxy{{ 9}}ethyl-2-oxo-1 ,2,3,{14}}Tetralin.
5. Lub cev qhuav dej ntawm 17-hydroxy-7-ethyl-2-oxo-1,2,3,4-tetrahydronaphthalene kom tau txais 17-methyl{{9 }}ethyl-1,2,3,{13}} Tetralin.
6. Epoxidation ntawm 17-methyl-7-ethyl-1,2,3,4-tetrahydronaphthalene kom tau txais 17-hydroxy-6 , {{9} }epoxy-17-methyl-1,2,3,{14}}tetrahydronaphthalene.
7. 17-Hydroxy-6 , 7 -epoxy-17-methyl-1,2,3,4-tetrahydronaphthalene tau deepoxidized kom tau txais {{9} }hydroxy-6 , 9 , 11 , 13 -tetrahydronaphthalene Methyl-1, 2,6,7,8,9,10,11,12,13,14,15,16,{ {27}}tetrahydrocyclopenta[a]phenanthrene-3-ib.
8. Rau 17-hydroxy-6 ,9 ,11 ,13 -tetramethyl-1,2,6,7,8,9,10,11,12,13,14 ,15,16,17-tetrahydrocyclo Penta[a]phenanthren-3-ib tug tau txais carbonylation los muab Clascoterone.
Cov tshuaj tiv thaiv tsuas yog hais txog ntau yam tshuaj lom neeg xws li alkylation, hydroxylation, oxidation, carbonyl txo, Lub cev qhuav dej, epoxidation, deepoxidation, thiab carbonylation. Cov kev mob tshwm sim no yuav tsum raug xaiv raws li cov xwm txheej tshwj xeeb, xws li kub, siab, catalyst, lub sijhawm tshuaj tiv thaiv thiab lwm yam, uas yuav tsis rov ua dua ntawm no.
Hauv kev xaus, cov txheej txheem hluavtaws ntawm Clascoterone muaj kev ua haujlwm siab thiab tawm los, thiab tuaj yeem paub txog kev tsim khoom loj. Vim nws cov qauv tshwj xeeb, nws yog qhov nyuaj rau kev sib txuas, uas tso siab rau cov kev xav tau ntau dua rau cov kws tshawb fawb chemists.
Clascoterone (lub npe lub npe Winlevi) yog cov tshuaj kho mob tshiab rau pob txuv me me. Nws yog ib qho tshuaj progesterone inhibitor uas ua rau cov androgen receptor, pob ntxau lub ntuj hormone, txo cov haujlwm ntawm cov qog sebaceous, yog li txo cov roj ntau lawm. Clascoterone muaj lwm yam kev siv ntxiv rau kev kho pob txuv, suav nrog:
1. Txiv neej qauv baldness: Clascoterone tuaj yeem siv los kho txiv neej qauv baldness, ib yam mob uas cuam tshuam rau cov plaub hau kev loj hlob ntawm cov txiv neej.
2. Top dandruff: Top dandruff yog ib yam kab mob dandruff uas ua rau dandruff, khaus, thiab poob ntawm cov plaub hau. Clascoterone yog siv los txo qhov mob, uas tuaj yeem txo cov tsos mob no.
3. Cov poj niam uas muaj plaub hau poob: Clascoterone kuj tseem siv los kho cov plaub hau poob ntawm cov poj niam, uas tuaj yeem tshwm sim los ntawm qib androgen siab.
4. Cov plaub hau loj hlob heev: Qee tus neeg yuav ntsib cov plaub hau loj hlob ntau dhau, uas yuav cuam tshuam rau cov tshuaj estrogen tsawg. Clascoterone ua haujlwm los ntawm inhibiting cov teebmeem ntawm androgens kom txo cov plaub hau ntau dhau.
Hauv kev xaus, Clascoterone yog ib qho tshuaj tshiab rau kev kho pob txuv thiab tuaj yeem siv los kho lwm yam kab mob, uas ua rau nws muaj peev xwm kho tau txhua yam tshuaj.
Clascoterone yog ib hom tshuaj antiandrogen tshiab rau kev kho pob txuv ntawm lub ntsej muag. Nws lub cev muaj zog muaj xws li: tsis muaj xim lossis lub teeb daj, me ntsis soluble hauv dej, yooj yim soluble hauv cov kuab tshuaj organic. Cov khoom siv tshuaj pom tau tias Clascoterone muaj cov qauv molecular ntawm C24H34O5 thiab molecular hnyav ntawm 410.5 g / mol. Hauv lub cev, nws tsuas yog ua tiav cov txiaj ntsig ntawm kev kho pob txuv los ntawm inhibiting androgen receptor hauv sebocytes.
Kev txhim kho keeb kwm ntawm Clascoterone yog qhov zoo siab heev. Nws tau tshawb pom thaum ntxov li xyoo 1960, tab sis kev npaj tau zoo tsis tau ua tiav. Txog thaum xyoo 2010, hauv kev sim tshuaj rau cov neeg mob pob txuv, qhov ua tau zoo ntawm Clascoterone tau pom tias yog qhov tseem ceeb heev. Thaum kawg, xyoo 2019, Clascoterone tau pom zoo los ntawm US FDA thiab dhau los ua lub hnub qub tshiab ntawm cov tshuaj kho pob txuv.
Txoj kev loj hlob zeem muag ntawm Clascoterone yog ci heev. Pob txuv yog ib yam kab mob uas tshwm sim thiab feem ntau cuam tshuam rau tib neeg lub ntsej muag thiab lub hlwb. Clascoterone, raws li ib qho kev kho mob hauv zos anti-androgen tshuaj, tsis tsuas yog cov nyhuv curative, tab sis kuj muaj kev nyab xeeb kev kho mob, uas tau txais kev saib xyuas thiab kev lag luam loj hlob. Yav tom ntej, Clascoterone yuav dhau los ua tus thawj coj hauv kev kho pob txuv, coj xov xwm zoo rau ntau pua lab tus neeg mob pob txuv. Nyob rau tib lub sijhawm, vim muaj cov khoom tiv thaiv androgenic ntawm Clascoterone, nws tseem tuaj yeem nrhiav tau ntau lub peev xwm hauv kev kho mob ntawm lwm yam kev mob androgen.