- PYRAZOLO[3,4-B]PYRIDINE COMPOUNDS, AND THEIR USE AS PHOSPHODIESTERASE INHIBITORS
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The invention relates to a compound of formula (I) or a salt thereof: wherein:R1 is C1-4alkyl, C1-3fluoroalkyl, -CH2CH2OH or -CH2CH2CO2C1-2alkyl;R2 is a hydrogen atom (H), methyl or C1fluoroalkyl;R3 is optionally substituted C3-8cycloalkyl or optionally substituted mono-unsaturated-C5-7cycloalkenyl or an optionally substituted heterocyclic group of sub-formula (aa), (bb) or (cc); in which n1 and n2 independently are 1 or 2; and in which Y is O, S, SO2, or NR10; or R3 is a bicyclic group (dd) or (ee): ; and wherein X is NR4R5 or OR5a. The compounds are phosphodiesterase (PDE) inhibitors, in particular PDE4 inhibitors. Also provided is the use of a compound of formula (I), or a pharmaceutically acceptable salt thereof, in the manufacture of a medicament for the treatment and/or prophylaxis of an inflammatory and/or allergic disease in a mammal such as a human, for example chronic obstructive pulmonary disease (COPD), asthma, or allergic rhinitis.
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- Application of N-Tritylmethionine in the Preparation of Heterocycles of Biological and Synthetic Interest
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Treatment of the methylsulfonium salts of the corresponding N-tritylmethionine derivatives with sodium hydride or potassium tert-butoxide provides the heterocycles N-trityl-L-homoserine lactone (3), (S)- and (R)-3-(N-tritylamino)tetrahydrofuran (7a, 7b), (S)-1-hydroxy-3-(N-tritylamino)-2-pyrrolidinone (14), (S)-4-(N-tritylamino)-1,2-oxazinan-3-one (15), (S)-3-(N-tritylamino)-2-pyrrolidone (23), (S)-1-tert-butyloxycarbonylamino-3-(N-tritylamino)-2-pyrrolidone (27), and (S)-2-methyl-4-(N-tritylamino)-1,2-oxazinan-3-one (18).Methylation of 14 and 15 yields (S)-1-methoxy-3-(N-tritylamino)-2-pyrrolidone (17) and 18, respectively.The stereochemistry of compounds 3, 7a, and 17 has been determined by X-ray crystal structure analysis.
- Barlos, Kleomenis,Papaioannou, Dionysios,Voliotis, Stavros
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p. 1127 - 1134
(2007/10/02)
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- Preparation of Optically Active Cyclic Ether Derivatives of Amino Acids and Peptides
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Treatment of N-tritylmethioninol (1) or peptides (6), incorporating methionyl and amino alcohol residues, with MeI, followed by base mediated cyclisation of the thus derived sulphonium salts, provides the title compounds in excellent yields.
- Barlos, Kleomenis,Papaioannou, Dionysios,Patrianakou, Stella,Sanida, Chariklia,Tsegenidis, Theodoros
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p. 474 - 475
(2007/10/02)
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