- A preparation method of generation of ralli department intermediates (by machine translation)
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The invention discloses a method for the preparation of generation of ralli department, aniline, N - Boc - L - 2 - aminobutyric acid, DCC, triethylamine, 2 - fluoro - 5 - nitrophenyl chloride as the raw material, through the condensation reaction, the ami
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Paragraph 0022; 0025
(2018/09/11)
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- A novel strategy for the manufacture of idelalisib: Controlling the formation of an enantiomer
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A novel and scalable synthesis of 5-fluoro-3-phenyl-2-[(1S)-1-(9H-purin-6-ylamino)propyl]-4(3H)-quinazolinone, idelalisib 1, has been developed. This strategy controls the desfluoro impurity of 13 during reduction of nitro intermediate 4, and also arrests the formation of the enantiomer during cyclisation of diamide 17, without affecting the neighbouring chiral centre. This process is demonstrated on a larger scale in the laboratory and achieved good chemical and chiral purities coupled with good yields.
- Mekala, Nagaraju,Buddepu, Srinivasa Rao,Dehury, Sanjay K.,Moturu, Krishna Murthy V. R.,Indukuri, Sunil Kumar V.,Vasireddi, Umamaheswara Rao,Parimi, Atchuta R.
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p. 15863 - 15869
(2018/05/04)
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- PROCESSES FOR PREPARATION OF IDELALISIB AND INTERMEDIATES THEREOF
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The present application provides processes for preparation of Idelalisib and intermediates thereof. The present application also provides a process for purification of Idelalisib.
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- Method for synthesizing [...]
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The invention relates to the technical field of anti cancer drug idelalisib, and especially relates to an idelalisib synthetic method which is as follows: taking 2-fluoro-6 nitro benzoic acid as a raw material for reacting with phenylamine to produce a compound III under the catalytic effect of a condensing agent; using N-boc-L-2-amino butyric acid as a raw material for reacting with the compound III to produce a compound V under the catalytic effect of a condensing agent; reducing the compound V by a metal or a metal compound and an acidic solution for cyclization to obtain a compound VI; removing the BOC group by protection group removal to obtain a compound VII; taking the compound VII and 6-bromo purine for nucleophilic reaction to obtain idelalisib. According to the method, a intermediate link of acyl chloride production is not needed, the operation process is simplified, time and labor cost are saved, the after-treatment is simple, the reaction yield is improved, cost is reduced, and the method has the advantages of being mild in reaction condition, high in yield, green and environmentally friendly, and meets the requirements of industrial production.
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- METHOD OF PREPARING 3-PHENYL-2-[9H-PURIN-6-YLAMINO)-METHYL]-3H-QUINAZOLIN-4-ONE AND SUBSTITUTED AND RELATED COMPOUNDS
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A method of synthesizing compounds of structural formulae (II), (IIa), and (III), in high yield and high stereospecific selectivity is disclosed. (IIa, R5≠H, S-enantiomer)
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Page/Page column 24; 26-27
(2010/02/14)
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