Naftifine hydrochloride

Naftifine hydrochloride 속성

Naftifine hydrochloride C화학적 특성, 용도, 생산

개요

Naftifine hydrochloride is a topical antifungal agent which acts via inhibiting squalene epoxidase. It demonstrates good activity against Trichophyton, Epidermophyton, Microsporum, Aspergillus, and species. It is the prototype of a significantly improved series of antifungal agents, exemplified by SF 86-327 in which the phenyl group of naftifine has been replaced by t-butylace tylene.

화학적 성질

White Powder

용도

An antifungal agent

일반 설명

N-Methyl-N-(3-phenyl2-propenyl)-1-naphthalenemethanaminehydrochloride (Naftin) is a white crystallinepowder that is soluble in polar solvents such asethanol and methylene chloride. It is supplied in a 1% concentrationin a cream and in a gel for the topical treatmentof ringworm, athlete’s foot, and jock itch. Although unapprovedfor these uses, naftifine has shown efficacy fortreatment of ringworm of the beard, ringworm of the scalp,and tinea versicolor.

Clinical Use

Naftifine hydrochloride (Naftin) is available for topical use only in the treatment of cutaneous dermatophyte and Candida infections; it is as effective as topical azoles for these conditions.

Synthesis

Naftifine hydrochloride is prepared by the reaction of (E)-N-methylcinnamylamine and 1-Chloromethylnaphthalene. The steps are as follows:
Step 1: (E)-N-methylcinnamylamine; 1-Chloromethylnaphthalene With sodium hydroxide In toluene at 86℃; for 6h;
Step 2: With hydrogenchloride In water; toluene at 15 - 20℃; for 3.5h；
Step 3: Add toluene (75 mL) to the yellow oil of step 2 (trans-N-cinnamomethylamine crude)And 15% NaOH (9.8g),Warming up,Stir well,When the temperature rises to 86 ° C,1-Chloromethylnaphthalene (11.8 g,100.2mmol), dripping,The reaction was incubated at 86 ° C for 6 h.Medium controlled N-cinnamylmethylamine is less than 0.5%,Cool down to 30 ° C, add water (75mL) to the system,Stirring and standing, separating the organic phase,The organic phase was washed with water (75 mL).Allow to stand and separate the organic phase, Concentrated hydrochloric acid (7.0 g) was added to the organic phase in a 15 ° C ice water bath.Adjust the pH to about 2 and stir for 0.5 h.After stirring at 20 ° C for 3 h, the filter cake was filtered.The filter cake was rinsed with toluene (20 mL).Obtained a wet cake (reduced naftifine hydrochloride) 19.5g;The wet crude product obtained in step 3 (crude naftifine hydrochloride) was added to isopropyl alcohol (38.6 g).Warmed to 85 ° C, dissolved,Slowly cool after dissolving,The cooling rate is 10 °C / h,A small amount of solid precipitated at 35 ° C.Crystallization at this temperature for 2 h,Continue to cool down to 20 ° C,Insulation for 3h,filter,Get the wet cake,The filter cake was dried under vacuum at 45 ° C.Obtained 16.2g of finished naftifine hydrochloride,The purity of the finished naftifine hydrochloride was 99.4% (HPLC normalization method).The product yield was 68.0%.The product yield is the molar yield,The calculation is as follows:Product yield (%)={m/[(m0/M0)*M]}*100%Symbol Description: m is the mass of the finished product, g; m0 is the mass of cinnamyl alcohol, g; M is the molar mass of naftifine hydrochloride,g/mol; M0 is the molar mass of cinnamyl alcohol, g/mol.

Naftifine hydrochloride 준비 용품 및 원자재

원자재

준비 용품

Naftifine hydrochloride 공급 업체

공급자	전화	이메일	국가	제품 수	이점
shandong perfect biotechnology co.ltd	+86-53169958659; +8618596095638	sales@sdperfect.com	China	294	58
Sinoway Industrial co., ltd.	0592-5800732; +8613806035118	xie@china-sinoway.com	China	992	58
Beijing Cooperate Pharmaceutical Co.,Ltd	010-60279497	sales01@cooperate-pharm.com	CHINA	1811	55
Henan Tianfu Chemical Co.,Ltd.	+86-0371-55170693 +86-19937530512	info@tianfuchem.com	China	21691	55
career henan chemical co	+86-0371-86658258	sales@coreychem.com	China	29914	58
Hubei Jusheng Technology Co.,Ltd.	18871490254	linda@hubeijusheng.com	CHINA	28180	58
Hubei xin bonus chemical co. LTD	86-13657291602	linda@hubeijusheng.com	CHINA	22968	58
Chongqing Chemdad Co., Ltd	+86-023-61398051 +8613650506873	sales@chemdad.com	China	39916	58
CONIER CHEM AND PHARMA LIMITED	+8618523575427	sales@conier.com	China	49390	58
Shaanxi Dideu Medichem Co. Ltd	18192627656	1012@dideu.com	China	3422	58

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