- PEPTIDE MACROCYCLES AGAINST ACINETOBACTER BAUMANNII
-
The present invention provides compounds of formula (I) wherein X1 to X8 and R1 to R8 are as described herein, as well as pharmaceutically acceptable salts thereof. Further the present invention is concerned with the manufacture of the compounds of formula (I), pharmaceutical compositions comprising them and their use as medicaments for the treatment of diseases and infections caused by Acinetobacter baumannii.
- -
-
Page/Page column 166
(2017/06/01)
-
- A 2-fluoro-3-chlorobenzene process for the preparation of formaldehyde
-
The invention relates to the field of fine chemical intermediates, in particular to a preparation method for 2-fluoro-3-chlorobenzaldehyde, namely, a fluorine-containing medical intermediate. According to the method, 2,3-dichlorobenzonitrile serves as raw materials, and 2-fluoro-3-chlorobenzaldehyde is obtained after fluorination, hydrolysis, oxidation and reduction are conducted. The method is low in raw material cost, high in apparent availability, mature and stable in reaction technology, high in operability and beneficial to industrial production.
- -
-
Paragraph 0059; 0060
(2017/03/08)
-
- Proton mobility in 2-substituted 1,3-dichlorobenzenes: "ortho" or "meta" metalation?
-
Nine 1,3-dichlorobenzene congeners were selected as model compounds to assess the relative rates of proton abstraction from 4- and 5-positions ("ortho" vs. "meta" metalation). Using lithium 2,2,6,6-tetramethylpiperidide as the basic reagent, the chlorine-adjacent 4-position underwent metalation exclusively. In contrast, attack at the chlorine-remote 5-posi" tion became significant even in the case of moderately sized 2-substituents (such as dimethylamino or ethyl) when secbutyllithium was employed. The "ortho/para" (4-/5-) ratios ranged from 80:20 to 65:35. The more pronounced "meta-orienting" effect of silicon as opposed to carbon substituents can be attributed to dissimilarities in the n polarization of the aromatic ring. Wiley-VCH Verlag GmbH & Co. KGaA, 2006.
- Schlosser, Manfred,Heiss, Christophe,Marzi, Elena,Scopelliti, Rosario
-
p. 4398 - 4404
(2007/10/03)
-
