- PYRAZOLOPYRIMIDINE DERIVATIVES USEFUL AS INHIBITORS OF BRUTON'S TYROSINE KINASE
-
This invention relates to compounds of formula (I). The compounds of the invention are tyrosine kinase inhibitors. Specifically, the compounds of the invention are useful as inhibitors of Bruton's tyrosine kinase (BTK). The invention also contemplates the
- -
-
Paragraph 00417-00418
(2016/01/01)
-
- Beyond directed ortho metalation: Ru-catalyzed CAr-O activation/cross-coupling reaction by amide chelation
-
Disclosed is a new, catalytic, and general methodology for the chemical synthesis of biaryl, heterobiaryl, and polyaryl molecules by the cross-coupling of o-methoxybenzamides with aryl boroneopentylates. The reaction is based on the activation of the unreactive C-OMe bond by the proximate amide directing group using catalytic RuH2(CO)(PPh3)3 conditions. A one-step, base-free coupling process is thereby established that has the potential to supersede the useful two-step directed ortho metalation/cross- coupling reaction involving cryogenic temperature and strong base conditions. High regioselectivity, orthogonality with the Suzuki-Miyaura reaction, operational simplicity, minimum waste, and convenient scale-up make these reactions suitable for industrial applications.
- Zhao, Yigang,Snieckus, Victor
-
supporting information
p. 11224 - 11227
(2014/09/29)
-
- Asymmetric synthesis of 3-substituted 8-hydroxy-3,4-dihydroisocoumarins from (S)-4-isopropyl-2-(2-methoxy-6-methylphenyl)oxazoline
-
Reaction of the laterally lithiated (S)-4-isopropyl-2-(2-methoxy-6-methylphenyl)oxazoline with p-tolualdehyde gave an inseparable mixture of the addition products in low diastereoselectivity. However, the (S,S)-product cyclized to the corresponding 3,4-di
- Uchida, Katsuya,Fukuda, Tsutomu,Iwao, Masatomo
-
p. 7178 - 7186
(2008/02/07)
-
- QUINAZOLINES USEFUL AS MODULATORS OF ION CHANNELS
-
The present invention relates to compounds useful as inhibitors of voltage-gated sodium channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.
- -
-
Page/Page column 189
(2008/06/13)
-
- Synthetic studies towards the benzophenone precursor for balanol
-
Synthesis of 4-carboxy-2,6-dimethoxyphenyl 2′-carboxy-6′- methoxyphenyl ketone, an important precursor for balanol's benzophenone portion, has been achieved via a short and efficient route in three steps using ortho-lithiation as the key step. In another
- Patil, Mahesh L.,Deshpande, Vishnu H.,Ramlingam,Borate, Hanumant B.
-
p. 1869 - 1873
(2007/10/03)
-
- Total synthesis of AI-77-B: Stereoselective hydroxylation of 4-alkenylazetidinones
-
A stereoselective synthesis of the anti-ulcer compound AI-77-B 1 is described. The 4-formylazetidinone 6 was converted into the 4-(Z)-alkene 23 using a phosphonate condensation, and dihydroxylation using osmium tetroxide and N-methylmorpholine W-oxide gav
- Broady, Simon D.,Rexhausen, Jost E.,Thomas, Eric J.
-
p. 1083 - 1094
(2007/10/03)
-
- A New Synthetic Route to 4-Bromo-7-methoxyphthalide and 3-Hydroxy-7-methoxyphthalide from 2-Methoxy-6-methylbenzoate Side Chain and Nuclear Bromination
-
Ethyl 2-methoxy-6-methylbenzoate was converted via its acid and acid chloride, into the methyl ester.Bromination of the methyl and ethyl esters with the halogen in carbon tetrachloride at reflux in the presence of light resulted in both side-chain and nuc
- Islam, Md. Rabiul,Joule, John A.
-
p. 367 - 378
(2007/10/02)
-
- Synthesis of Gerberinol-I
-
The synthesis of 4-hydroxy-5-methylcoumarin (II) is described.The compound (II) affords gerberinol-I (I) on treatment with formaldehyde.The synthetic sample of I is identical (m.m.p. and co-IR) with an authentic I.
- Chatterjea, J. N.,Singh, K. R. R. P.,Jha, I. S.,Prasad, Y.,Shaw, S. C.
-
p. 796 - 798
(2007/10/02)
-