Sapropterin

CAT#: H318853

CAS#: 62989-33-7 / 69056-38-8

Description: Sapropterin, also known as Tetrahydrobiopterin (BH4, THB, trade name Kuvan) or sapropterin (INN) is a naturally occurring essential cofactor of the three aromatic amino acid hydroxylase enzymes, used in the degradation of amino acid phenylalanine and in the biosynthesis of the neurotransmitters serotonin (5-hydroxytryptamine, 5-HT), melatonin, dopamine, norepinephrine (noradrenaline), epinephrine (adrenaline), and is a cofactor for the production of nitric oxide (NO) by the nitric oxide synthases. Chemically, its structure is that of a reduced pteridine derivative.

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Synthetic Routes

Sapropterin - Synthetic Route 1

Sapropterin route01

Synthetic reference

Lyudnikova, T. A.; Dashina, O. A.; Telegina, T. A.; Kritsky, M. S. Investigation of the photochemical properties of biopterin and its reduced forms. Applied Biochemistry and Microbiology. Volume 45. Issue 1. Pages 104-109. 2009.

Sapropterin - Synthetic Route 2

Sapropterin route02

Synthetic reference

Moser, Rudolf; Groehn, Viola; Schumacher, Andreas; Martin, Pierre. Preparation of tetrahydrobiopterin and analogs of tetrahydrobiopterin. Assignee BioMarin Pharmaceutical Inc., USA; Merck Eprova A.-G. WO 2005049614. (2005).

Sapropterin - Synthetic Route 3

Sapropterin route03

Synthetic reference

Matsuura, Sadao; Murata, Shizuaki; Sugimoto, Takashi. Hydrogenation of biopterin and its analogs; application for the convenient procedure of biopterin cofactor and related 5,6,7,8-tetrahydropterins. Heterocycles. Volume 23. Issue 12. Pages 3115-20. 1985.

Sapropterin - Synthetic Route 4

Sapropterin route04

Synthetic reference

Yoshino, Hiroshi; Kiyono, Hiroomi. Process for the preparation of R-sapropterin. Assignee Shiratori Pharmaceutical Co., Ltd., Japan. JP 2009298754. (2009).

Sapropterin - Synthetic Route 5

Sapropterin route05

Synthetic reference

Hong, Hao; Gage, James; Chen, Chaoyong; Lu, Jiangping; Zhou, Yan; Liu, Shuangyong. Method for synthesizing sapropterin dihydrochloride. Assignee Asymchem Laboratories (Tianjin) Co., Ltd., Peop. Rep. China; Asymchem Life Science (Tianjin) Co., Ltd.; Tianjin Asymchem Pharmaceutical Co., Ltd.; Asymchem Laboratories (Fuxin) Co., Ltd.; Jilin Asymchem Laboratories Co., Ltd. WO 2013152609. (2013).

Sapropterin - Synthetic Route 6

Sapropterin route06

Synthetic reference

Henderson, Mark; Jungles, Steven; Roidl, Gabriele; Baffi, Robert; Indolese, Adriano; Mueller, Christian; Schmidt, Philipp; Kaiser, Stefan. Method of synthesizing tetrahydrobiopterin from diacetylbiopterin. Assignee BioMarin Pharmaceutical Inc., USA. WO 2009088979. (2009).

Sapropterin - Synthetic Route 7

Sapropterin route07

Synthetic reference

Wang, Zhen; Zhao, Dongbing; Wang, Weida; Lan, Jingbo; You, Jingsong. Preparation process of (6R)-tetrahydrobiopterin hydrochloride. Assignee InnoPharmax, Inc., Peop. Rep. China. WO 2012048451. (2012).

Sapropterin - Synthetic Route 8

Sapropterin route08

Synthetic reference

Prasad, Konakanchi Durga; Buchappa, Gongalla; Babu, Kotra Uma Naresh; Babu, Sikha Kotaiah; Srinivasulu, Sakkani; Nagamani, Brahmadevi; Murthy, Konduri Srinivasa Krishna; Kumar, Remella Ravi; Kumar, Thoota Sandeep; Chandrasekhar, Javvadi; Reddy, Muddasani Pulla; Rao, Adibhatla Kali Satya Bhujanga; Chaudhary, Nannapaneni Venkaiah. Novel process for the preparation of sapropterin dihydrochloride and its key intermediate, L-biopterin. Assignee Natco Pharma Limited, India. IN 2015CH02684. (2016).

Sapropterin - Synthetic Route 9

Sapropterin route09

Synthetic reference

Wu, Fujian. Preparation method for sapropterin hydrochloride. Assignee Beijing Cavir Bio-Pharm Co., Ltd., Peop. Rep. China; Suzhou Zhiyu Biotechnology Co., Ltd. WO 2016101211. (2016).

Sapropterin - Synthetic Route 10

Sapropterin route010

Synthetic reference

Wang, Chen; Chao, Tung-Ping; Wang, Wei-Ta; Lan, Ching-Po; Yu, Chin-Sung. Preparation process of (6R)-tetrahydrobiopterin hydrochloride. Assignee InnoPharmax, Inc., Taiwan. CN 102443006. (2012).