Indole Synthesis by Controlled Carbolithiation of o-Aminostyrenes
摘要:
An effective synthesis of the functionalized indole ring system has been developed from substituted o-aminostyrene starting material. Our methodology involves a novel cascade reaction sequence of alkyllithium addition to the styrene double bond and subsequent trapping of the intermediate organolithium with a suitable electrophile, followed by an in situ ring closure and dehydration to generate the indole ring. This new reaction sequence allows for the introduction of molecular diversity at all positions on the indole scaffold. The procedure was shown to be successful with a range of both C and N substituents on the o-aminostyrenes. The reaction sequence was tolerant to the reactivity range of alkyllithiums such as tert-, sec-, and n-butyllithium. The electrophiles used were DMF, which generated indole products with C-2 unsubstituted, and nitriles, which incorporated the nitrile substituent at C-2. The o-aminostyrene starting materials were generated by a Pd-catalyzed cross-coupling reaction of a vinyl boronic acid equivalent with the readily available substituted o-bromoanilines.
Catalytic reduction of aromatic ring in aqueous medium
申请人:King Fahd University of Petroleum and Minerals
公开号:US10618878B1
公开(公告)日:2020-04-14
A method of reducing an aromatic ring under relatively mild condition using sub-nano particles of a transition metal supported on super paramagnetic iron oxide nanoparticles (SPIONs). The catalyst is efficient for catalyzing the reduction of both carbocyclic and heterocyclic compound. In compound comprising both carbocyclic and heterocyclic aromatic rings, the catalyst displays high regioselectivity for the heterocyclic ring.
The present disclosure relates to stimulators of soluble guanylate cyclase (sGC), pharmaceutical formulations comprising them and their uses thereof, alone or in combination with one or more additional agents, for treating various diseases, wherein an increase in the concentration of nitric oxide (NO) or an increase in the concentration of cyclic Guanosine Monophosphate (cGMP), or both, or an upregulation of the NO pathway is desirable. The compounds are of Formula I:
PIPERAZINE-SUBSTITUTED BENZOTHIOPHENES FOR TREATMENT OF MENTAL DISORDERS
申请人:Otsuka Pharmaceutical Co., Ltd.
公开号:US20130158044A1
公开(公告)日:2013-06-20
The present invention provides a heterocyclic compound represented by the general formula (1): The compound of the present invention has a wide treatment spectrum for mental disorders including central nervous system disorders, no side effects and high safety.
A process for addition polymerisation of vinylic (in particuar methacrylic) monomers at a temperature in the range of -20 to 60°C, in the presence of a catalyst comprising:
(a) a first component of empirical formula (I):
wherein
M is an alkali metal atom; and
T is bulky hydrocarbyl which contains at least 4 carbon atoms and is optionally substituted by one or more pendent substituents, or hetero-substituted hydrocarbyl, each of which is inert in the process conditions; and
(b) a (co-catalyst) second component comprising a compound of empirical formula (II):
wherein
Q is Al, B or Zn;
m, n and p are each 0 or an integer such that (m + n + p) = 2 or 3 (depending on the appropriate valency of Q; and
X, Y and Z are each independently optionally substituted bulky hydrocarbyl, or
X and Y together are optionally substituted hydrocarbadiyl, and Z is optionally substituted bulky hydrocarbyl,
all of which groups are inert in the process conditions.
在催化剂存在下,乙烯基(特别是甲基丙烯酸)单体在-20-60℃温度范围内进行加成聚合的工艺,包括
(a) 经验式 (I) 的第一组分:
其中
M 是碱金属原子;和
T 是含有至少 4 个碳原子且任选被一个或多个下垂取代基取代的笨重烃基,或杂取代烃基,其中每个取代基在工艺条件下都是惰性的;以及
(b) 由经验式(II)化合物组成的(助催化剂)第二组分:
其中
Q 是 Al、B 或 Zn
m、n 和 p 各为 0 或整数,使得 (m + n + p) = 2 或 3(取决于 Q 的适当价数;以及
X、Y 和 Z 各自独立地是任选取代的笨重烃基,或
X 和 Y 共同为任选取代的烃基,Z 为任选取代的笨重烃基、
所有这些基团在加工条件下均为惰性。
Water-developable photosensitive composition and production process thereof
申请人:Nippon Paint Co., Ltd.
公开号:EP0859284A1
公开(公告)日:1998-08-19
The present invention provides a water-developable photosensitive composition capable of providing a flexographic printing plate with a satisfactory shelf life, excellent water developability, water resistance, ink resistance and aging resistance, as well as an adequate impact resilience necessary for a high evenness of the reproduced image, and a production process thereof.
A water-developable photosensitive composition comprising (A) a thermoplastic elastic polymer, (B) an ionic group- and photopolymerizable double bond-containing hydrophilic polymer, (C) a crosslinking particulate resin having an ionic group capable of forming an ion pair with said polymer (B), and (D) a photopolymerization initiator.