Bosutinib Monohydrate Chemische Eigenschaften,Einsatz,Produktion Methoden

Definition

ChEBI: A hydrate that is the monohydrate form of anhydrous bosutinib.

Clinical Use

Bosulif ® (Bosutinib hydrate), also known as (SKI-606), is a novel 4-phenylamino-3-quinolinecarbonitrile kinase inhibitor approved for treatment of adults with chronic, accelerated, or blast phase Philadelphia chromosome-positive chronic myeloid leukemia (Ph+CML). Bosutinib is an orally-dosed, dual Src/Abl kinase inhibitor which provides an alternative treatment to patients exhibiting immunity to imatinib and other kinase inhibitors utilized for this treatment. In contrast to competitor tyrosine inhibitors, bosutinib inhibits autophosphorylation of both Srs and Abl kinases, leading to decreased cell growth and apoptosis. Bosutinib was originally developed by Wyeth and continues to be marketed by Pfizer after the merger of Wyeth and Pfizer in 2009.

Synthese

Several synthetic routes to bosutinib have been reported, including synthetic work for scale up and processing to obtain pure salt forms of bosutinib for pharmaceutical applications.56-59 The current manufacturing route begins with reaction of 2-methoxy-5-nitrophenol (36) and 1-bromo-3- chloropropane (37) to provide aryl chloroether 38 in 82% yield. Reaction of 38 with Nmethylpiperazine (39) and NaI in refluxing DME provided the functionalized aryl-nitro-piperazine 40 (77% yield), which was converted directly to aniline 41 under hydrogenolysis conditions. Aniline 41 was then reacted with triethyl orthoformate and aryl cyanoamide 42, which was generated in one step from 2,4-dichloro-5-methoxy-aniline (44), 1,3-diisopropylcabodiimide (DIC), and cyanoacetic acid (45) under refluxing conditions, to yield advanced intermediate 43 (93% over 2 steps). Finally, conversion of 43 to bosutinib was facilitated by a POCl3-promoted cyclization in the presence of sulfolane. As shown in Scheme 8, employment of carefully optimized conditions for the isolation of bosutinib hydrate (VII) provided material in 75-82% yields and >99% purity.

Bosutinib Monohydrate Upstream-Materialien And Downstream Produkte

Upstream-Materialien

Downstream Produkte

Bosutinib Monohydrate Anbieter Lieferant Produzent Hersteller Vertrieb H?ndler.

Firmenname	Telefon	E-Mail	Land	Produktkatalog	Edge Rate
ATK CHEMICAL COMPANY LIMITED	+undefined-21-51877795	ivan@atkchemical.com	China	32951	60
career henan chemical co	+86-0371-86658258 +8613203830695	sales@coreychem.com	China	29885	58
Zhejiang ZETian Fine Chemicals Co. LTD	+8618957127338	stella@zetchem.com	China	2136	58
Chongqing Chemdad Co., Ltd	+86-023-6139-8061 +86-86-13650506873	sales@chemdad.com	China	39894	58
Shanghai Jinghao Pharmaceutical Co.,Ltd	+86-21-68900963	sales@jinghaopharma.com	CHINA	153	58
Shanghai Yingrui Biopharma Co.,Ltd	21-33585366	export01@shyrchem.com	CHINA	1319	58
TargetMol Chemicals Inc.	+1-781-999-5354 +1-00000000000	marketing@targetmol.com	United States	32072	58
Hubei Ipure Biology Co., Ltd	+8613367258412	ada@ipurechemical.com	China	10319	58
AFINE CHEMICALS LIMITED	+86-0571-85134551	sales@afinechem.com	China	15356	58
Baoji Guokang Healthchem co.,ltd	+8615604608665 15604608665	dominicguo@gk-bio.com	CHINA	9414	58

---

• Bosutinib Monohydrate
• bosutinib hydrate
• Bosutinib MonohydrateQ: What is Bosutinib Monohydrate Q: What is the CAS Number of Bosutinib Monohydrate
• 4-((2,4-Dichloro-5-methoxyphenyl)amino)-6-methoxy-7-(3-(4-methylpiperazin-1-yl)propoxy)quinoline-3-carbonitrile hydrate
• 918639-08-4
• C26H31Cl2N5O4
• C26H29Cl2N5O3H2O