- The studies on chemoselective promiscuous activity of hydrolases on acylals transformations
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Chemoselective, mild and convenient protocol for the hydrolysis of the synthetically relevant acylals via promiscuous enzyme-catalyzed hydrolysis has been developed. It has been shown that promiscuous activity of the used hydrolases dominates their native activity related with carboxylic esters hydrolysis. The main advantage of the present methodology is that it can be conducted under neutral conditions at room temperature. Moreover, complete deprotection of acylals takes place within 10–20 min. Developed protocol can be used with compounds having a variety of hydrolytic labile groups since the cleavage is proceeded under neutral conditions and occurs exclusively on acylal moiety. Further this protocol was extended by the tandem Passerini multicomponent reaction leading to the α-acetoxy amides using acylals as the surrogates of the carbonyl components to P-MCR.
- Koszelewski, Dominik,Ostaszewski, Ryszard
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- Copper(I)-catalyzed hydroalkoxylation/hydrogen-bonding-induced asymmetric hetero-diels-alder cycloaddition cascade: An approach to aromatic spiroketals
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One thing leads to another: Bis(benzannelated) 5,6-spiroketal skeletons can be constructed by an efficient cascade process involving an unprecedented CuI-catalyzed intramolecular alkyne hydroalkoxylation and an asymmetric hetero-Diels-Alder cyc
- Li, Xin,Xue, Jijun,Huang, Chusheng,Li, Ying
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supporting information; experimental part
p. 903 - 906
(2012/07/03)
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- Molecular iodine in isopropenyl acetate (IPA): a highly efficient catalyst for the acetylation of alcohols, amines and phenols under solvent free conditions
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Iodine in isopropenyl acetate (IPA) is a highly efficient catalyst for the acetylation of a variety of alcohols, phenols and amines under solvent free conditions. Primary, secondary, tertiary alcohols, amines and mono to polyhydroxy phenols and anilines with electron donating or withdrawing substituents can be easily acetylated in good to excellent yield at 85-90 °C.
- Ahmed, Naseem,van Lier, Johan E.
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p. 5345 - 5349
(2007/10/03)
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- Convenient synthesis of a simple coumarin from salicylaldehyde and wittig reagent. IV: Improved synthetic method of substituted coumarins
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The reaction of salicylaldehydes (2) with Horner-Wadsworth-Emmons (HWE) or Ando-HWE reagents was attempted to afford intramolecular phosphonate derivatives (6). A new synthetic method for coumarins (1) was achieved by using protected 2.
- Takeuchi, Yasuo,Ueda, Norihiro,Uesugi, Koji,Abe, Hitoshi,Nishioka, Hiromi,Harayama, Takashi
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p. 217 - 224
(2007/10/03)
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- Non-steroid progesterone receptor agonist and antagonist and compounds and methods
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Non-steroidal compounds which are high affinity, high specificity ligands for progesterone receptors are disclosed. The compounds include synthetic derivatives of cyclocymopol and its diastereomers, spectroscopically and chromatographically pure (3R)-cyclocymopol monomethyl ether, which functions as a progesterone receptor antagonist, and spectroscopically and chromatographically pure (3S)-cyclocymopol monomethyl ether, which functions as a progesterone receptor agonist. Also disclosed are methods for employing the disclosed compounds for modulating processes mediated by progesterone receptors and for treating patients requiring progesterone receptor agonist or antagonist therapy.
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- Non-steroid androgen receptor antagonist compounds and methods
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Non-steroidal compounds which are high affinity, high specificity ligand antagonists for the androgen receptor are disclosed. Also disclosed are methods for employing the disclosed compounds for modulating processes mediated by the androgen receptor and for treating patients requiring androgen receptor antagonist therapy.
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