409346-73-2Relevant articles and documents
B(C6F5)3-catalyzed divergent cyanosilylations of chromones dependent on temperature
Wang, Qiaotian,Feng, Xiangqing,Meng, Wei,Du, Haifeng
, p. 8354 - 8357 (2019/09/30)
A B(C6F5)3-catalyzed divergent cyanosilylation of chromones has been successfully realized. A variety of 4-oxochromane-2-carbonitriles were furnished as kinetic products in high yields via 1,4-cyanosilylations. An unexpected C-O bond cyanosilylation was achieved when the temperature was raised to 80 °C, affording 4-oxo-4-(2-hydroxylphenyl)but-2-enenitriles as thermodynamic products in 72-94% yields, which was confirmed by DFT results.
Preparation method and application of Smo inhibitor based on Nebivolol
-
, (2019/10/17)
The invention discloses a preparation method and an application of a Smo inhibitor based on Nebivolol. The structural formula of the Smo inhibitor is as shown in a formula (I). The invention further discloses a synthetic method and an application of the Smo inhibitor. According to the Smo inhibitor, a beta-receptor retardant Nebivolol with inhibitory activity for Smo proteins serves as a lead compound, and optimization reconstruction is implemented based on the beta-receptor retardant Nebivolol to obtain the Smo inhibitor with good inhibitory activity.
Preparation method of 6-fluorochromane-2-formaldehyde as nebivolol intermediate
-
Paragraph 0012, (2017/08/28)
The invention discloses a preparation method of 6-fluorochromane-2-formaldehyde used as a key intermediate of nebivolol for treating essential hypertension. At the temperature of 50 to 80 DEG C, 6-fluorochromane-2-methanol is dissolved in a solvent, in oxygen atmosphere, 2,2,6,6-tetramethyl-1-piperidinyloxy (TEMPO), cuprous bromide, 2,2-bipyridine and N-methylimidazole (NMI) are catalytically reacted to obtain 6-fluorochromane-2-formaldehyde. The synthetic method of 6-fluorochromane-2-formaldehyde used as the nebivolol intermediate provided by the invention is mild in reaction condition and simple to operate; the product purity LC of 6-fluorochromane-2-formaldehyde can reach 95%, the yield of 6-fluorochromane-2-formaldehyde is 82% or more, and the used catalysts are environment-friendly and suitable for industrial production.
PROCESS FOR PREPARATION OF NEBIVOLOL AND IT'S SALTS
-
Page/Page column 13; 14, (2016/12/07)
The present invention discloses a new process for preparation of Nebivolol or it's pharmaceutically acceptable salt. More particularly, the invention discloses an improved economical process for the preparation of intermediate, 6-fluoro-3,4- dihydro-2H-1-benzopyran-2-carboxaldehyde of Formula – II, converting the 6- fluoro-3,4-dihydro-2H-1-benzopyran-2-carboxaldehyde of Formula – II into mixture of [R*(S*)]-6-fluoro-3,4-dihydro-2-oxiranyl-2H-1-benzopyran and [R*(R*)]-6-fluoro-3,4-dihydro-2-oxiranyl-2H-1-benzopyran of Formula-V and separation of diastereomers of (R*)-6-Fluoro-3,4-dihydro-2-((S*)-oxiran-2-yl)- 2H-benzopran by forming azeotrope.
A PROCESS FOR THE PREPARATION OF 6-FLUORO-3,4-DIHYDRO-2H-CHROMENE- 2-CARBALDEHYDE
-
Page/Page column 6; 7, (2014/08/06)
The present invention relates to a process for ihe preparation of 6-f!uoro-3,4-dihydro- 2H-chromene-2-carbaidehyde which is useful as an Intermediate in the synthesis of Nebivolol or its pharmaceutical acceptable salts.
PREPARATION OF NEBIVOLOL
-
, (2011/10/19)
Processes for the synthesis of pharmacologically active 2,2-iminobisethanol derivatives, e.g., 2H-1-benzopyran-2 methanol-α,α′-iminobis(methylene)]bis-[6-fluoro-3,4-dihydro-[2R*[R*[R*(S*)]]]], and their pharmaceutically acceptable salts.
NEBIVOLOL AND ITS PHARMACEUTICALLY ACCEPTABLE SALTS, PROCESS FOR PREPARATION AND PHARMACEUTICAL COMPOSITIONS OF NEBIVOLOL
-
Page/Page column 12; 16; 33, (2010/10/20)
The present invention provides an improved process for the synthesis of nebivolol or its pharmaceutically acceptable salts, more particularly hydrochloride salt of formula (I). The present invention further provides a new Form T1 of nebivolol and its pharmaceutically acceptable salts. The present invention also provides pharmaceutical compositions and process for the preparation of a solid oral dosage form of nebivolol hydrochloride of formula (I), without the use of wetting agent, and optionally using binder and /or disintegrant.
A mild synthesis of α,α′-[iminobismethylene]bis[6-fluoro- 3,4-dihydro-2H-1 -benzopyran-2-methanol]
Bai, Yihui,Chen, Xinzhi
, p. 807 - 808 (2007/10/03)
A new synthesis of α,α′-[iminobismethylene]bis[6-fluoro- 3,4-dihydro-2H-1-benzopyran-2-methanol (1) is described, with most reactions being carried out at room temperature and normal pressure, that will further contribute to the development of new scalable synthesis of the related drug substance of Nebivolol (overall yield: 33%).
Metabotropic glutamate receptor antagonists
-
, (2008/06/13)
The present invention concerns compounds of formula. In a preferable embodiment, X represents O; R1 represents C1-6alkyl; cycloC3-12alkyl or (cycloC3-12alkyl)C1-6alkyl, wherein one or more hydrogen atoms in a C1-6alkyl-moiety or in a cycloC3-12alkyl-moiety optionally may be replaced by C1-6alkyloxy, aryl, halo or thienyl; R2 represents hydrogen; halo; C1-6alkyl or amino; R3 and R4 each independently represent hydrogen or C1-6alkyl; or R2 and R3 may be taken together to form —R2-R3-, which represents a bivalent radical of formula -Z4-CH2-CH2-CH2- or -Z4-CH2-CH2- with Z4 being O or NR11 wherein R11 is C1-6alkyl; and wherein each bivalent radical is optionally substituted with C1-6alkyl; or R3 and R4 may be taken together to form a bivalent radical of formula —CH2-CH2-CH2-CH2-; R5 represents hydrogen; Y represents O; and aryl represents phenyl optionally substituted with halo. The invention also relates to the use of a compound according to the invention as a medicament and in the manufacture of a medicament for treating or preventing glutamate-induced diseases of the central nervous system, as well as formulations comprising such a compound and processes for preparing such a compound.
