Bosutinib Monohydrate
- CAS No.
- 918639-08-4
- Chemical Name:
- Bosutinib Monohydrate
- Synonyms
- bosutinib hydrate;Bosutinib Monohydrate;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
- CBNumber:
- CB62728577
- Molecular Formula:
- C26H31Cl2N5O4
- Molecular Weight:
- 548.47
- MOL File:
- 918639-08-4.mol
- Modify Date:
- 2024/7/2 8:55:13
SAFETY
Risk and Safety Statements
| Symbol(GHS) |   GHS07,GHS09 |
|---|---|
| Signal word | Warning |
| Hazard statements | H400-H410-H317 |
| Precautionary statements | P273-P391-P501-P273-P391-P501-P261-P272-P280-P302+P352-P333+P313-P321-P363-P501 |
Bosutinib Monohydrate Chemical Properties,Uses,Production
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.
Synthesis
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 Preparation Products And Raw materials
Raw materials
Preparation Products
| Supplier | Tel | Country | ProdList | Advantage | Inquiry |
|---|---|---|---|---|---|
| Alembic Pharmaceuticals Limited | +91-2652280880 +91-2652280550 | Gujarat, India | 115 | 58 | Inquiry |
| MSN LABORATORIES PRIVATE LTD | +91 40 30438600 | New Delhi, India | 230 | 58 | Inquiry |
| CLEARSYNTH LABS LTD. | +91-22-45045900 | Hyderabad, India | 6351 | 58 | Inquiry |
| Pharmaffiliates Analytics and Synthetics P. Ltd | +91-172-5066494 | Haryana, India | 6773 | 58 | Inquiry |
| SynZeal Research Pvt Ltd | +1 226-802-2078 | Gujarat, India | 6522 | 58 | Inquiry |
| Pharma Affiliates | 172-5066494 | Haryana, India | 6761 | 58 | Inquiry |
| ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 | China | 32760 | 60 | Inquiry |
| career henan chemical co | +86-0371-86658258 +8613203830695 | China | 29898 | 58 | Inquiry |
| Zhejiang ZETian Fine Chemicals Co. LTD | +8618957127338 | China | 2141 | 58 | Inquiry |
| Chongqing Chemdad Co., Ltd | +86-023-6139-8061 +86-86-13650506873 | China | 39916 | 58 | Inquiry |
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