- RAPAMYCIN ANALOGS AND USES THEREOF
-
The present invention provides compounds, compositions thereof, and methods of using the same.
- -
-
Paragraph 00549-00550
(2020/01/08)
-
- FUSED [1,2,4]THIADIAZINE DERIVATIVES WHICH ACT AS KAT INHIBITORS OF THE MYST FAMILY
-
A compound of formula (I): which inhibits the activity of one or more KATs of the MYST family, i.e., TIP60, KAT6B, MOZ, HBO1 and MOF.
- -
-
Page/Page column 73
(2019/03/17)
-
- A Study on the Intramolecular Mitsunobu Reaction of N6-(ω-Hydroxyalkyl)adenines
-
The cyclization of N6-(ω-hydroxyalkyl)adenines with a N6H-group leads to N6,N1 ring closure regardless of the method of the cyclization that was used. Five-membered to eight-membered rings were obtained using NBS/PPh3; however, under Mitsunobu conditions, the eight-membered fused purine was not formed. Surprisingly, the cyclization of N6-methyl-N6-(4-hydroxybutyl)adenine only leads to N6,N7 ring closure using both methods.
- ?im?nková, Nadě?da,Tobrman, Tomá?,Eigner, Václav,Dvo?ák, Dalimil
-
p. 3565 - 3573
(2017/11/21)
-
- VALSARTAN DERIVATIVES CARRYING NITROGEN OXIDE DONORS FOR THE TREATMENT OF VASCULAR AND METABOLIC DISEASES
-
Nitrate esters and diazeniumdiolate derivatives of valsartanamide are described. They have valuable properties in the treatment of vascular and metabolic diseases.
- -
-
Page/Page column 14
(2011/11/06)
-
- A valsartanamide dinitrate derivative for the treatment of vascular and metabolic diseases
-
A dinitrate ester of a valsartanamide is described. It has superior properties in the treatment of vascular and metabolic diseases.
- -
-
Page/Page column 7
(2011/11/01)
-
- A mild and facile synthesis of cyclic imides using pyridinium chlorochromate
-
A mild and facile synthetic method of cyclic imides is presented. These compounds are widely used in the synthesis of novel medical, polymeric, photonic and electronic materials. Compared with traditional syntheses, the method reported has several advantages including mild conditions, simplified work-up and low cost.
- Yang, Yanyan,Wang, Ge,Cao, Xiaohui,Yan, Xilong,Chen, Ligong
-
p. 657 - 658,2
(2020/07/30)
-
- Desymmetrization of meso-cyclic imides via enantioselective monohydrogenation
-
meso-Cyclic imides are monohydrogenated to form the corresponding hydroxy lactams in 88-97% ee using trans-[Ru((R)-BINAP)(H)2((R,R)-dpen)] and related compounds as catalysts with base in THF. The hydrogenation proceeds with high enantiogroup-and chemoselectivity, and it is a desymmetrization reaction, forming up to five stereogenic centers in one reaction. Conversion of a hydroxy lactam into the corresponding iminium ion followed by addition of indene extended the number of stereogenic centers from 5 to 7.
- Takebayashi, Satoshi,John, Jeremy M.,Bergens, Steven H.
-
supporting information; experimental part
p. 12832 - 12834
(2010/11/03)
-
- PHOSPHADIAZINE HCV POLYMERASE INHIBITORS I AND II
-
Provided herein are phosphadiazine polymerase inhibitor, for example, of any of Formula I, II, III, I′, II′, I″, II″, Ia, IIa, or IIIa, pharmaceutical compositions comprising the compounds, and processes of preparation thereof. Also provided are methods of their use for the treatment of an HCV infection in a host in need thereof.
- -
-
Page/Page column 67
(2009/04/24)
-
- PROCESS FOR THE PREPARATION OF N-AKYL-PYRROLIDONES
-
A process for the production of N-alkylpyrrolidone from γ-butyrolactone and monoalkylamine in the liquid phase comprising the steps of: feeding monoalkylamine and γ-butyrolactone, in the absence of water or in the presence of less than about 1 wt % of water, to a reaction zone to form a reaction mixture; heating the reaction mixture; withdrawing a product stream from the reaction zone and passing the stream to a distillation zone comprising at least one distillation column operated at sub-atmospheric pressure; adding water to the distillation zone; isolating at least one overhead stream from the distillation zone comprising monoalkylamine, water and optionally N-alkyl-pyrrolidone and condensing the overhead stream against cooling water.
- -
-
Page/Page column 9
(2008/06/13)
-
- Methods of making intermediates from polyhydroxyalkanoates
-
Methods of forming intermediates from PHAs are disclosed.
- -
-
-
- Preparation of N-methyl-2-pyrrolidone (NMP)
-
N-Methyl-2-pyrrolidone (NMP) is prepared by preparing a mixture comprising monomethylamine, dimethylamine and trimethylamine and ammonia in a first process step by reacting ammonia with methanol at elevated temperature in the presence of a catalyst, separating 10 off the ammonia, reacting the mixture comprising the methylamines with gamma-butyrolactone (γ-BL), in a molar ratio of monomethylamine to γ-BL of at least 1 in a second process step at elevated temperature and superatmospheric pressure, separating NMP and unreacted methylamines from the reaction product and returning unreacted methylamines to the first process step for reaction with methanol and ammonia.
- -
-
Page column 6
(2008/06/13)
-
- A novel method for the preparation of nucleoside diphosphates
-
Figure presented Sugar nucleoside diphosphates have been prepared using an efficient phosphate coupling reaction that employs a highly reactive zwitterionic phosphoramidate intermediate as the phosphorylating species.
- Freel Meyers, Caren L.,Borch, Richard F.
-
p. 3765 - 3768
(2007/10/03)
-
- Preparation of N-methy1-2-pyrrolidone (NMP)
-
N-Methyl-2-pyrrolidone (NMP) is prepared by preparing a mixture comprising monomethylamine, dimethylamine and trimethylamine and ammonia in a first process step by reacting ammonia with methanol at elevated temperature in the presence of a catalyst, separating off the ammonia, reacting the mixture comprising the methylamines with gamma-butyrolactone (γ-BL), in a molar ratio of monomethylamine to γ-BL of at least 1 in a second process step at elevated temperature and superatmospheric pressure, separating NMP and unreacted methylamines from the reaction product and returning unreacted methylamines to the first process step for reaction with methanol and ammonia.
- -
-
-
- The 4-[N-methyl-N-(2,2,2-trifiuoroacetyl)amino]butyl group as an alternative to the 2-cyanoethyl group for phosphate protection in the synthesis of oligodeoxyribonucleotides
-
The 4-[N-methyl-N-(2,2,2-trifluoroacetyl)amino]butyl group for phosphate protection in the synthesis of oligodeoxyribonucleotides has been developed to completely prevent nucleobase alkylation by acrylonitrile that could potentially occur upon deprotection of the traditional 2-cyanoethyl phosphate protecting group. The properties of this new phosphate protecting group were evaluated using the model phosphotriester 9. The mechanism of phosphate deprotection was studied by treating 9 with concentrated NH4OH. NMR analysis of the deprotection reaction demonstrated that cleavage of the N- trifiuoroacetyl group is rate-limiting. The resulting phosphotriester intermediate 13 was also shown to undergo rapid cyclodeesterification to produce O,O-diethyl phosphate 15 and N-methylpyrrolidine 16 (Scheme 2). Given the facile removal of the 4-[N-methyl-N-(2,2,2-trifluoroacetyl)amino]butyl phosphate protecting group under mild basic conditions, its utilization in oligonucleotide synthesis began with the preparation of the deoxyribonucleoside phosphoramidites 4a-d (Scheme 3). The coupling efficiency of 4a-d and conventional 2-cyanoethyl deoxyribonucleoside phosphoramidites 24a-d was then compared in the solid-phase synthesis of the 20-met d(ATCCGTAGCTAAGGTCATGC). As previously observed in the deprotection of 9, the 4-[N-methyl,N-(2,2,2-trifluoroacetyl)amino]butyl phosphate protecting groups were easily and completely removed from the oligonucleotide by using either concentrated NH4OH or pressurized ammonia gas. Analysis of the deprotected oligomer by polyacrylamide gel electrophoresis (Figure 3) indicated that the phosphoramidites 4a-d are as efficient as the 2-cyanoethyl phosphoramidites 24a-d in the synthesis of the 20-mer. Furthermore, following digestion of the crude 20-met by snake venom phosphodiesterase and bacterial alkaline phosphatase, HPLC analysis showed complete hydrolysis to individual nucleosides and no detectable nucleobase modification.
- Wilk, Andrzej,Grajkowski, Andrzej,Phillips, Lawrence R.,Beaucage, Serge L.
-
p. 7515 - 7522
(2007/10/03)
-