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Published synthesis of PD-0332991 (Palbociclib) Essay Example

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Published synthesis of PD-0332991 (Palbociclib)

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The preferred range of temperature is between 60oC to 90oC (the range is important to keep the enzymatic reaction optimum, besides, this range attains the desired speed without altering the expected results), which is maintained for 10 hours. After the process, the intermediate ester formed undergoes the cyclization process through AcOH and heating.This stage involves amino-pyridinyl Coupling. The stage begins with the halogenation of the compound from the previous stage. The halogenation process involves taking the compound through several conditions. It involves the addition of bromide compounds. The process involves using a suitable solvent and a base. The heating stage continues for 16 hours while stirring at a temperature between 40oC to 60o C. Example of base include the sodium acetate while solvents such as acetic acids require duration of 35 hours at a temperature of 50oc. Other bases with a potential for the similar purpose include potassium acetate while the solvents such sdichlroromethane and methanol may also be used ( because they provide optimal medium for the reaction similar to the primary solvent) as alternative to this process. The preferred agents for the halogenation process include the dibromohydantoin, NBS, or bromine.The step involve using organosilicon compound named lithium bis(trimethylsilyl)amide-LiHMDS, which act as a ligand. The ligand reacts with the bromine halide (attached to the comound) through a process called salt metathesis reaction (as shown in the figure 7 below). The process give rise to a meta trimethylsilyl amide, which makes the compound lipophilic (because of the effect by the ligand). The product formed will be soluble in the non polar solvents hence increasing its reactivity.This stage is called regioselective Heck Coupling. The stage involves using a suitable solvent like n-butanol (because the complex has increased reactivity with n-butanol unlike other non polar solvents), which is mixed with a base and vinyl ether. Prior to the commencement of heating the mixture, usually at a temperature of 75oC, a catalyst of palladium is added (as shown in figure 8 below). The process is maintained for about 10 hours while stirring the mixture.The final stage involve adding isethionic acid and carrying out deprotection. The process of adding isethionic acid uses a specific protocol. The whole step last for about 1 hour with optimal results expected after 3

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preview essay on Published synthesis of PD-0332991 (Palbociclib)
  • Pages: 4 (1000 words)
  • Document Type: Essay
  • Subject: Chemistry
  • Level: Undergraduate
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