Naloxegol Oxalate Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung

Naloxegol oxalate (XXI) is a peripherally acting μ-opioid receptor antagonist that was approved in the USA and EU for the treatment of opioid-induced constipation in adults with chronic non-cancer pain. The drug, a pegylated version of naloxone, has significantly reduced central nervous system (CNS) penetration and works by inhibiting the binding of opioids in the gastrointestinal tract. Naloxegol oxalate was developed by Nektar and licensed to AstraZeneca. Although we were unable to find a single report in the primary or patent literature that describes the exact experimental procedures to prepare naloxegol oxalate, there have been reports on the preparation of closely related analogs with specific reports on improving the selectivity of the reduction step156 and the salt formation of the final drug substance.

Verwenden

Naloxegol Oxalate is an oxalate form of Naloxegol (N284470) which is a peripherally-selective opioid antagonist.

Synthese

Naloxone (180) was treated with methoxyethyl chloride in the presence of Hunigˉs base to give the protected ketone 181. Reduction of the ketone with potassium trisec- butylborohydride exclusively provided the a-alcohol 182 in 85% yield. Alternatively, sodium trialkylborohydrides could also be used to provide similar a-selective reduction in high yield. Deprotonation of the alcohol with sodium hydride followed by alkylation with CH3(OCH2CH2)7Br (183) provided the pegylated intermediate 184 in 88% yield. Acidic removal of the methoxyethyl ether protecting group followed by treatment with oxalic acid and crystallization provided naloxegol oxalate (XXI) in good yield.

Naloxegol Oxalate Upstream-Materialien And Downstream Produkte

Upstream-Materialien

Downstream Produkte

Naloxegol Oxalate Anbieter Lieferant Produzent Hersteller Vertrieb H?ndler.

Firmenname	Telefon	E-Mail	Land	Produktkatalog	Edge Rate
Hebei Chuanghai Biotechnology Co., Ltd	+8615531151365	mina@chuanghaibio.com	China	18126	58
BEIJING SJAR TECHNOLOGY DEVELOPMENT CO., LTD.	+86-18600796368	sales@sjar-tech.com	China	529	58
Henan Tianfu Chemical Co.,Ltd.	+86-0371-55170693 +86-19937530512	info@tianfuchem.com	China	21586	55
ATK CHEMICAL COMPANY LIMITED	+undefined-21-51877795	ivan@atkchemical.com	China	33024	60
Hebei Yanxi Chemical Co., Ltd.	+8618531123677	faithe@yan-xi.com	China	5853	58
TargetMol Chemicals Inc.	+1-781-999-5354; +17819995354	marketing@targetmol.com	United States	32466	58
HANGZHOU CLAP TECHNOLOGY CO.,LTD	86-571-88216897,88216896 13588875226	sales@hzclap.com	CHINA	6312	58
BOC Sciences	16314854226; +16314854226	inquiry@bocsci.com	United States	19853	58
InvivoChem	+1-708-310-1919 +1-13798911105	sales@invivochem.cn	United States	6391	58
TargetMol Chemicals Inc.	+1-781-999-5354;	support@targetmol.com	United States	39039	58

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• Naloxegol Oxalate
• Naloxegol Oxalate NKTR-118
• (5alpha,6alpha)-4,5-Epoxy-6-(3,6,9,12,15,18,21-heptaoxadocos-1-yloxy)-17-(2-propen-1-yl)-morphinan-3,14-diol ethanedioate
• AZ 13337019 oxalate
• NKTR 118 oxalate
• (4R,4aS,7S,7aR,12bS)-7-[2-[2-[2-[2-[2-[2-(2-methoxyethoxy)ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]-3-prop-2-enyl-1,2,4,5,6,7,7a,13-octahydro-4,12-methanobenzofuro[3,2-e]isoquinoline-4a,9-diol,oxalic acid
• Naloxegol oxalate salt
• Naloxegol OxalateQ: What is Naloxegol Oxalate Q: What is the CAS Number of Naloxegol Oxalate Q: What is the storage condition of Naloxegol Oxalate
• NKTR-118;NKTR118;NKTR 118
• (4R,4aS,7S,7aR,12bS)-7-[2-[2-[2-[2-[2-[2-(2-methoxyethoxy)ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]-3-prop-2-enyl-1,2,4,5,6,7,7a,13-octahydro-4,12-methanobenzofuro[3,2-e]isoquinoline-4a,9-diol
• Morphinan-3,14-diol,4,5-epoxy-6-(3,6,9,12,15,18,21-heptaoxadocos-1-yloxy)-17-(2-propen-1-yl)-,(5α,6α)-,ethanedioate(1:1)(salt)
• NKTR-118
• Morphinan-3,14-diol, 4,5-epoxy-6-(3,6,9,12,15,18,21-heptaoxadocos-1-yloxy)-17-(2-propen-1-yl)-, (5α,6α)-, ethanedioate (1:1)
• Naloxone oxalate
• 1354744-91-4
• C34H53NO11C2H2O4