Monday, July 24, 2017

Reliable manufacturers of posaconazole and its intermediates

Posaconazole

Posaconazole is a triazole antifungal drug, marketed by Schering-Plough. It is a derivative of Itraconazole.
Generic Name: posaconazole
Brand Name: Noxafil, Posanol
Indications, Side Effects, Warnings Consumer Information of posaconazole please refer to: www.drugs.com

Chemical information of posaconazole:
CAS#: 171228-49-2
Chemical name:4-[4-[4-[4-[[(3R,5R)-5-(2,4-Difluorophenyl)-5-(1,2,4-triazol-1-ylmethyl)oxolan-3-yl]methoxy]phenyl]piperazin-1-yl]phenyl]-2-[(2S,3S)-2-hydroxypentan-3-yl]-1,2,4-triazol-3-one
Chemical structure:
Posaconazole.svg
List of manufacturers approved for Generic posaconazole: none

List of manufacturers applied DMF for posaconazole: (by June 2017, data from www.fda.gov):
1. SANDOZ PRIVATE LTD (2010)
2. MSN LABORATORIES PRIVATE LTD (2013)
3. WUHAN ZY PHARMACEUTICAL CO LTD (2014)
4. BRIGHTGENE BIOMEDICAL TECHNOLOGY CO LTD (2014)
5. MSN LABORATORIES PRIVATE LTD (2015)
6. ZHEJIANG AUSUN PHARMACEUTICAL CO LTD(2016)
7. APOTEX PHARMACHEM INC (2016)
8. STRIDES SHASUN LTD (2017)

List of manufacturers of posaconazole in China (data from www.sfda.gov.cn):
1. Nanjing Zhengke
2. Jiangsu Hengsheng
3. Jiangsu Aosaikang
4. Chongqing Huabang Shengkai
5. Xinxiang Shuanglu
6. Henan Tailong
7. Shanghai Xiandai
8. Hebei Guolong
9. Jichuan Pharma
10. Wuhan Zhongyou
11. Shanxi Zhendong
12. Jiangsu Shengdi
13. Jiangsu Haici Bio-pharm
14. Chengdu Beite
15. Shanxi Pude

Intermediates of posaconazole:
Advanced posaconazole intermediates:
1. CAS# 175712-02-4 :(5R-cis)- p-Chlorobenzenesulfonic acid 5-(2,4-difluoro-
phenyl)-5-[1,2,4]triazol-1-ylmethyl-tetrahydro-furan-3-ylmethyl ester
Chemical structure:
posaconazole intermediate 1
2. CAS# 184177-83-1 : 2-[(1S,2S)-1-ethyl-2-bezyloxypropyl]-2,4-dihydro-4-[4-[4-(4-hydroxyphenyl)-1-piperazinyl]phenyl]- 3H-1,2,4-Triazol-3-one
Chemical structure: posaconazole intermediate 2
Other posaconazole intermediates:
3. CAS# 170985-85-0 :((2S,3S)-2-(benzyloxy)pentan-3-yl)hydrazinecarboxaldehyde
Chemical structure:posaconazole intermediate 2-1
4. CAS# 184177-81-9 : phenyl N-[4-[4-(4-hydroxyphenyl)piperazin-1-yl]phenyl]carbamate
Chemical structure:posaconazole intermediate 2-2
5. CAS# 183871-36-5 : ((2S,3S)-2-(benzyloxy)pentan-3-yl)hydrazine dibenzoyl-D-tartrate
Chemical structure:posaconazole intermediate 2-1-1
6. CAS# 74853-08-0 : 1-(4-Aminophenyl)-4-(4-hydroxyphenyl)piperazine
Chemical structure:posaconazole intermediate 2-2-1
7. CAS#149809-43-8: (5R-cis)-Toluene-4-sulfonic acid 5-(2,4-difluoro-phenyl)-5-[1,2,4]triazol-1-ylmethyl-tetrahydro-furan-3-ylmethyl ester
Chemical structure: 


Manufacturers of posaconazole intermediates:

1. Brightgene Biomedical
2. Langfang Gaobo
3. Pingdingshan Chemiway
4. Zhangjiakou Gerui
......

* For detailed information or contact information of posaconazole manufacturers, please leave message or send email to: michaelapci@gmail.com
ROS: Synthesis of Posaconazole for reference:

Title:Tetrahydrofuran antifungals
Authors:Saksena, A.K.; Girijavallabhan, V.M.; Lovey, R.G.; Pike, R.E.; Wang, H.; Liu, Y.-T.; Ganguly, A.K.; Bennett, F. (Schering Corp.)
Source:EP 0736030; JP 1997500658; US 5661151; US 5703079; WO 9517407

Drugs similar with posaconazole: 
Itraconazole (1992, Janssen)
Itraconazole.svg


fluconazole (1988, Pfizer)
Fluconazole skeletal formula.svg
Voriconazole (2002, Pfizer)
Voriconazole structure.svg
Isavuconazole (2015, Basilea, Astellas ),
Isavuconazonium sulfate.svg


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