- PROCESS AND INTERMEDIATES FOR THE PREPARATION OF BILASTINE
-
The invention relates to a process for preparing a compound of (III) wherein X is a leaving group; and R1 is C1-C6 alkyl; which comprises oxidative rearrangement of a compound of formula (II) or a solvate thereof Compounds of formula (III) are key intermediates in the synthesis of Bilastine.
- -
-
Page/Page column 19-20
(2020/02/16)
-
- Preparation method of bilastine intermediate
-
The invention discloses a preparation method of a bilastine intermediate, and relates to the technical field of organic matter synthesis. The bilastine intermediate is a compound 2. The preparation method comprises the following steps: carrying out a substitution reaction on a compound 3, halogenated acetyl halide and aluminum trihalide in an organic solvent, directly adding 1,1,3,3-tetramethyldisiloxane (TMDS) into a reaction solution after the reaction is finished, carrying out a reduction reaction, and dropwise adding the reaction solution into water after the reaction is finished in orderto carry out a quenching reaction. The substitution reaction of the compound 3 and chloroacetyl chloride and the carbonyl reduction reaction of the compound 4 can be carried out by a one-pot method, the TMDS is directly added after the reaction of the first step is finished, the quenching reaction is carried out after the reaction of the second step is finished, the heat release of the quenching reaction is not obvious, and the experiment safety is improved; and in the second-step reaction, 1,1,3,3-tetramethyldisiloxane is adopted, strict anhydrous conditions are not needed, the operation is simple and convenient, and the reaction conditions are mild.
- -
-
Paragraph 0029-0030; 0033-0034; 0036
(2020/05/02)
-
- A new and competitive synthetic approach for an antihistamine agent, bilastine
-
Efforts towards the novel synthesis of second generation non-sedating antihistamine drug, Bilastine was described in this manuscript. This competitive synthetic approach involves the convergent synthesis of Bilastine via simple Friedel-Crafts acylation as an alternate for earlier reported Stille and Suzuki couplings. The selectivity in Friedel-Crafts acylation reaction with chloro acetyl chloride on different substituted arenes was studied and employed the best conditions for the synthesis of Bilastine. Further synthetic approach involves the deoxygenation of aryl ketone to corresponding alkane in single step and finally provides Bilastine with 39% of improved overall yields, utilizing simple and cost-effective reagents, suitable for kilogram scale synthesis.
- Kommera, Rajashekar,Yerrabelly, Jayaprakash Rao,Kasireddy, Venkateshwarreddy,Ghojala, Venkat Reddy,Singavarapu, Adilakshmi,Rebelli, Pradeep
-
p. 815 - 821
(2018/11/06)
-
- NOVEL PROCESS FOR THE PREPARATION OF 2-[4-(2-{4-[1-(2-ETHOXYETHYL)-1H-BENZIMIDAZOL-2-YL]-1-PIPERIDINYL}ETHYL) PHENYL]-2-METHYLPROPANOIC ACID
-
The present invention relates to novel process for the preparation of 2-[4-(2-{4-[l-(2- ethoxyethyl)-lH-benzimidazol-2-yl]-l-piperidinyl}ethyl)phenyl]-2-methylpropanoic acid represented by the following structural formula- 1. Formula- 1 The present invention also provides novel intermediate compounds useful for the preparation of compound of formula- 1.
- -
-
Page/Page column 27; 28
(2014/12/12)
-