- COMBINATION TREATMENTS COMPRISING ADMINISTRATION OF 1H-PYRAZOLO[4,3-B]PYRIDINES
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The present invention provides 1H-pyrazolo[4,3-b]pyridin-7-amines of formula (I) as PDE1 inhibitors together with a second compound useful in the treatment of a neurodegenerative disorder and their combined use as a medicament, in particular for the treatment of neurodegenerative and/or cognitive disorders.
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Page/Page column 119
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- COMBINATION TREATMENTS COMPRISING ADMINISTRATION OF 1H-PYRAZOLO[4,3-B]PYRIDINES
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The present invention provides 1H-pyrazolo[4,3-b]pyridin-7-amines of formula (I) as PDE1 inhibitors together with a second compound which compound is useful in the treatment of a psychiatric disorder and their combined use as a medicament, in particular for the treatment of psychiatric and/or cognitive disorders.
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Page/Page column 115-116
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- 1H-PYRAZOLO[4,3-B]PYRIDINES AS PDE1 INHIBITORS
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The present invention provides 1H-pyrazolo[4,3-b]pyridin-7-amines of formula (I) as PDE1 inhibitors and their use as a medicament, in particular for the treatment of neurodegenerative disorders and psychiatric disorders.
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Page/Page column 110
(2018/09/25)
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- Synthesis of cyclic N-nitrourethanes by the simultaneous oxidative desulfurization and nitration of cyclic thiourethanes
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The reaction of five- and six-membered cyclic thiourethanes with acetyl nitrate results in a vigorous reaction that generates copious amounts of red-brown nitrogen oxide fumes and produces the corresponding cyclic N-nitrourethanes in high yields (>95%). The overall yield of the cyclic N-nitrourethanes starting from an aminoalcohol using the " thiourethane" route is superior to the conventional route going through the cyclic urethane. Copyright
- Willer, Rodney L.,Campbell, Christopher G.,Storey, Robson F.
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scheme or table
p. 421 - 423
(2012/06/18)
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- Synthesis of some 2-Oxazolidinones in mild conditions
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One step efficient protocol for the synthesis of 2-oxazolidinones in paste chemical medium is described under microwave activation with 80 % yield.
- Bratulescu, George
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experimental part
p. 929 - 930
(2011/12/15)
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- A novel way to chiral 2-oxazolidinones: selenium-catalyzed cyclocarbonylation of 2-aminoethanols
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Selenium-catalyzed cyclocarbonylation of 2-aminoethanols with CO under atmospheric pressure at 30 °C afforded 2-oxazolidinones in excellent yields without any other co-catalyst. The method was then applied to the syntheses of chiral 2-oxazolidinones and no racemization was detected.
- Li, Peng,Yuan, Xiaohua,Wang, Shudong,Lu, Shiwei
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p. 12419 - 12423
(2008/03/13)
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- Synthesis of 2-oxazolidinones by salen-Co-complexes catalyzed oxidative carbonylation of β-amino alcohols
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2-Oxazolidinones are synthesized in high yield by oxidative carbonylation of β-amino alcohols using salen-Co(II)/NaI or salen-Co(III)-I as a catalyst and using CO as the carbonyl source. Studies of functional group compatibility using a series of substituted salen-Co(II) or salen-Co(III)-I complexes demonstrate a broad tolerance of functionality during the carbonylation reaction.
- Liu, Jian-Ming,Peng, Xin-Gao,Liu, Jian-Hua,Zheng, Shu-Zhan,Sun, Wei,Xia, Chun-Gu
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p. 929 - 932
(2008/02/04)
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- A novel and efficient (NHC)CuI (NHC = N-heterocyclic carbene) catalyst for the oxidative carbonylation of amino compounds
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Oxidative carbonylation of amino compounds to prepare corresponding 2-oxazolidinones, ureas, and carbamates selectively in the presence of (NHC)CuI without any additives was firstly achieved in good yields and selectivities.
- Zheng, Shuzhan,Li, Fuwei,Liu, Jianming,Xia, Chungu
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p. 5883 - 5886
(2008/02/09)
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- Efficient synthesis of oxazolidin-2-one via (chitosan-Schiff base)cobalt(II)-catalyzed oxidative carbonylation of 2-aminoalkan-1-ols
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The (chitosan-Schiff base)cobalt(II) complex was found to be an efficient catalyst for the oxidative carbonylation (CO/O2) of 2-aminoalkan-1-ols 1 to give oxazolidin-2-ones 2, in the presence of NaI. The effects of promoters, temperature, solvents, and other reaction conditions were investigated in this study.
- Liu, Jianming,Sun, Wei,Zheng, Shuzhan,Xia, Chungu
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p. 1593 - 1598
(2008/02/09)
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- Pd(Phen)Cl2 stabilized by ionic liquid: an efficient and reusable catalyst for biphasic oxidative cyclocarbonylation of β-aminoalcohols and 2-aminophenol
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Biphasic oxidative cyclocarbonylation of β-aminoalcohols and 2-aminophenol to synthesize corresponding 2-oxazolidinones were investigated in the presence of ionic liquid stabilized Pd(phen)Cl2 complex. Catalytic comparison results showed that, 1-butyl-3-methyl-imidazolium iodide salts (BMImI) can serve simultaneously as a specific stabilizer to protect the transition metal complex against deactivation, a promoter to increase the catalytic performance and a reaction medium to recycle the catalyst with unprecedented TOF value.
- Li, Fuwei,Xia, Chungu
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p. 4845 - 4848
(2008/02/05)
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- Silver-catalyzed intermolecular amination of C-H groups
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(Chemical Equation Presented) Teamwork: The dinuclear silver complex [Ag2(OTf)2(bp)2] (OTf = trifluoromethane- sulfonate, bp = bathophenanthroline) catalyzes the intermolecular amination of saturated C-H bonds by using Phl=NNs (Ns = p-nitrosulfonyl) as the nitrene precursor (see scheme). Preliminary investigations suggest that the dinuclear structural motif is crucial to catalytic performance.
- Li, Zigang,Capretto,Rahaman,He, Chuan
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p. 5184 - 5186
(2008/03/18)
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- A highly efficient sulfur-catalyzed oxidative carbonylation of primary amines and β-amino alcohols
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A highly efficient sulfur-catalyzed oxidative carbonylation of aliphatic amines and aliphatic β-amino alcohols to ureas and 2-oxazolidinones, respectively, was developed. Sodium nitrite was involved in the reoxidation of hydrogen sulfide to sulfur in the catalytic oxidative carbonylation cycle. Georg Thieme Verlag Stuttgart.
- Peng, Xingao,Li, Fuwei,Xia, Chungu
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p. 1161 - 1164
(2007/10/03)
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- Modified Mg: Al hydrotalcite in the synthesis of oxazolidin-2-ones
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The modified Mg: Al (3: 1) hydrotalcite has been found to be an efficient catalyst in the conversion of carbamates into oxazolidin-2-ones under mild reaction conditions. A wide variety of oxazolidin-2-ones were obtained with excellent chemical yield. The Royal Society of Chemistry 2005.
- Cwik, Agnieszka,Fuchs, Aliz,Hell, Zoltan,Boejtoes, Ildiko,Halmai, Dora,Bombicz, Petra
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p. 967 - 969
(2007/10/03)
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- Synthesis of 2-oxazolidinone catalyzed by palladium on charcoal: A novel and highly effective heterogeneous catalytic system for oxidative cyclocarbonylation of β-aminoalcohols and 2-aminophenol
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Oxidative cyclocarbonylation of β-aminoalcohols and 2-aminophenol to synthesize corresponding 2-oxazolidinones catalyzed by a Pd/C-I2 heterogeneous catalytic system has been developed which gave excellent selectivity and high turnover frequency (TOF) values 15 times larger than the best results previously reported. The catalyst could be reused for five times almost without losing its catalytic activity and selectivity. The effects of promoters, pretreatment, solvents, and reaction conditions have been investigated.
- Li, Fuwei,Xia, Chungu
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p. 542 - 546
(2007/10/03)
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- A silver-catalyzed intramolecular amidation of saturated C-H bonds
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Opportunities with silver: A dinuclear silver(I) compound was found to efficiently catalyze the intramolecular amidation of saturated C-H bonds of carbamates and sulfamates (see scheme). This highly regioselective, stereospecific reaction offers a practical method for the construction of cyclic nitrogen-containing organic molecules.
- Cui, Yong,He, Chuan
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p. 4210 - 4212
(2007/10/03)
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- Chemical fixation of carbon dioxide co-catalyzed by a combination of Schiff bases or phenols and organic bases
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Binaphthyldiamino, ethyldiamino and cyclohexyldiamino Schiff bases can catalyze the reaction of epoxides with carbon dioxide in the presence of catalytic amounts of various organic bases to give the corresponding cyclic carbonates in high yields. The simplest binaphthyldiamino Schiff base, derived from the reaction of binaphthyldiamine with salicylaldehyde, gave the highest yield of cyclic carbonate. This catalytic system can be further simplified by use of a phenol instead of the Schiff base to give the corresponding cyclic carbonates in high yields as well. Mechanistic insights were obtained based on a deuterium labeling experiment, The reaction of aziridines with CO2 and epoxide with CS2 were also examined under the same reaction conditions. Wiley-VCH Verlag GmbH & Co. KGaA, 69451 Weinheim, Germany, 2004.
- Shen, Yu-Mei,Duan, Wei-Liang,Shi, Min
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p. 3080 - 3089
(2007/10/03)
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- New Routes to Chiral Evans Auxiliaries by Enzymatic Desymmetrisation and Resolution Strategies
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This paper describes how enantiomerically enriched Evans auxiliaries can be successfully prepared by either an enzymatic desymmetrisation strategy or an asymmetric synthesis using racemic auxiliaries and an enzymatic resolution. Desymmetrisation of N-Boc-protected serinol has been achieved in good yield and high enantiomeric excess using porcine pancreas lipase. This has been exploited in different ways to prepare enantiomerically enriched (4R)- and (4S)-substituted 2-oxazolidinones. In another approach to asymmetric synthesis, starting from a racemic Evans auxiliary, by means of a diastereoselective aldol reaction coupled with a lipase-catalysed resolution, we achieved the preparation of enantiomerically enriched β-hydroxy acids and enantiomerically enriched 2-oxazolidinones.
- Neri, Claudia,Williams, Jonathan M. J.
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p. 835 - 848
(2007/10/03)
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- Synthesis of chiral oxazolidin-2-ones by 1,2-amino alcohols, carbon dioxide and electrogenerated acetonitrile anion
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An improved electrochemical synthesis of chiral oxazolidin-2-ones from chiral 1,2-amino alcohols is obtained by direct electrolysis of solutions of MeCN-TEAP containing the amino alcohol, with subsequent CO2 bubbling and addition of TsCl. This
- Feroci, Marta,Gennaro, Armando,Inesi, Achille,Orsini, Monica,Palombi, Laura
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p. 5863 - 5865
(2007/10/03)
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- Synthesis of 2-oxazolidones by sulfur-assisted thiocarboxylation with carbon monoxide and oxidative cyclization with molecular oxygen under mild conditions
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Simple synthetic method on 2-oxazolidone derivatives was established. 2-Aminoethanols were easily subjected to the thiocarboxylation with carbon monoxide promoted by elemental sulfur, followed by the oxidative cyclization with molecular oxygen to give corresponding 2-oxazolidones in good yields under mild conditions (1 atm, rt). Furthermore, 2-imidazolidones and 2-thiazolidone were also prepared in good yields similarly.
- Mizuno, Takumi,Takahashi, Junko,Ogawa, Akiya
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p. 7805 - 7808
(2007/10/03)
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- A Rh-catalyzed C-H insertion reaction for the oxidative conversion of carbamates to oxazolidinones
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Selective intramolecular alkane oxidations: an RhII carboxylate catalyzed C-H amination reaction facilitates the preparation of 1,2-amino alcohols from primary carbamates. The reaction is stereospecific, providing access to chiral α-branched amines from optically pure starting with no loss in enantiomeric excess (see scheme).
- Espino, Christine G.,Du Bois
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p. 598 - 600
(2007/10/03)
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- Synthesis of 2-Oxo-Oxazolidines and -Thiazolidines from the Corresponding 2-Thioxo Compounds
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2-Thioxo-oxazolidines and -thiazolidines are easily converted by reaction with an epoxide under acidic conditions into the corresponding 2-oxo compounds.
- Calo, Vinzenzo,Nacci, Angelo,Volpe, Angela
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p. 283 - 286
(2007/10/03)
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- Chiral Dipole-Stabilized Anions: Experiment and Theory in Benzylic and Allylic Systems. Stereoselective Deprotonations, Pyramidal Inversions, and Stereoselective Alkylations of Lithiated (Tetrahydroisoquinolyl)oxazolines
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The stereoselective alkylation of chiral (tetrahydroisoquinolyl)oxazolines has been investigated.We report the details of this investigation, including an examination of the effect of both temperature and oxazoline substituent structure on the alkylation diastereoselectivity, a comparison of monodentate vs bidentate chelation of the organolithium, an evaluation of the effect of solvent and chelating solvent additives, the regiochemistry of alkylation of (3,4-dehydropiperidino)oxazolines, lithiation-alkylation experiments on stereoselectively deuterated monodentate and bidentate isoquinolinolyloxazolines, and semiempirical molecular orbital calculations on the organolithium diastereomers 13a,b.There are two distinct stereoselective processes involved in the overall transformation. the proposed mechanism includes an oxazoline-alkyllithium coordination complex that controls the selectivity of the deprotonation step, whereas the selectivity of the electrophilic quench is governed by effects that are as yet undetermined.
- Rein, Kathleen,Goicoechea-Pappas, Marta,Anklekar, Tarakeshwar V.,Hart, Georgina C.,Smith, Gregory A.,Gawley, Robert E.
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p. 2211 - 2217
(2007/10/02)
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- PREPARATION OF CYCLIC CARBONATES AND 2-OXAZOLIDONES USING DI-2-PYRIDYL CARBONATE
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Cyclic carbonates and 2-oxazolidones are conveniently prepared in high yields by the reaction of diols and β-amino alcohols with di-2-pyridyl carbonate.It is of synthetic significance that the formation of cyclic carbonates in refluxing toluene occurs under essentially neutral conditions.
- Kim, Sunggak,Ko, Young Kwan
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p. 1625 - 1630
(2007/10/02)
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