A practical
synthetic route of belinostat is reported. Belinostat
was obtained via a five-step process starting from benzaldehyde and
including addition reaction with sodium bisulfite, sulfochlorination
with chlorosulfonic acid, sulfonamidation with aniline, Knoevenagel
condensation, and the final amidation with hydroxylamine. Key to the
strategy is the preparation of 3-formylbenzenesulfonyl chloride using
an economical and practical protocol. The main advantages of the route
include inexpensive starting materials and acceptable overall yield.
The scale-up experiment was carried out to provide 169 g of belinostat
with 99.6% purity in 33% total yield.
A practical synthetic route to pimavanserin tartrate, in which the target compound was obtained with 99.84% purity and in 46% total yield via a 5-step synthesis starting from 4-hydroxybenzaldehyde and (4-fluorophenyl)methanamine, is reported. The main advantages of the route include inexpensive starting materials, mild reaction conditions and an acceptable overall yield.
This study designed a handheld vibrating coffee harvester to improve the mechanized harvesting of Coffea arabica L. The proposed device was used to vibrate branches of Coffea arabica L. trees, and the shedding of coffee fruit and the operation parameters of vibrational harvesting were analyzed. Images captured using high-speed photography were used to derive a force equation that represents the forced vibration of the coffee fruit-stalk joint. In addition, the vibrations of coffee berries and branches were theoretically analyzed, and the results were used to establish a dynamic vibration model of coffee trees. The shedding of coffee berries was primarily affected by the vibration frequency, vibration amplitude, and excitation position, which were simulated using a rigid–flexible branch-machine coupling model on RecurDyn software. Furthermore, field experiments were conducted to determine the optimal working parameters for coffee harvesting using vibrations. The results indicated optimal picking performance when the vibration frequency, vibration amplitude, and excitation position were 62 Hz, 9 mm, and 0.4 L, respectively. The harvesting rates of ripe and unripe coffee were 92.22% and 8.33%, respectively, and the damage rate was 5.23%. Thus, the proposed harvester can satisfactorily achieve the optimal harvesting of Coffea arabica L.
A synthetic route to 3-formylbenzenesulfonyl chloride derivatives from the corresponding benzaldehydes has been developed. The key step in this procedure is the conversion of aldehyde bisulfite adducts to target compounds via a two-stage reaction in the presence of Na2SO4. A series of 3-formylbenzenesulfonyl chloride derivatives were prepared by this method and identified by chemical derivatization method.
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