The Half Decent Pharmaceutical Chemistry Blog

Of course, if you don't live in Europe, the title will lose all its sense but, come on, use some imagination!
This is the first synthesis here, and I opted for an important drug, Prazosin, mainly used in the treatment of hypertension: an alpha-1-adrenergic antagonist.

This molecule is the lead for other quinazoline derivatives such as doxazosin and cyclazosin.

Here is the synthesis:

This is not totally synthetic, so, if you know a more sophisticated version of this synthesis, please, I'd love to know where I can find it. (I mean, I'm still an undergrad).

For what concerns this synthesis, it's certainly not a complicated one. The very first step involves sodium cyanate and yields a product which can remind of a ketene.
Phosphoroxidchloride is used as chlorinating agent.
I'd like to point out that it's due to thermodynamic reasons that we substitute one Cl only (how lucky, eh?)

The most interesting aspect is the way we yield the furanyl-piperazinyl-methanone. We set pH at 5.5, because the two NH groups in the piperazine have different basicity and this, plus the great reactivity of the furan-2-carbonyl chloride, would lead to double substituted products (hence, a mixture of three products). Thanks to this particular pH, you may say, we protect one of the NH functions and we increase selectivity.

Today it should have been the beginning of the discussion of pharmaceutical syntheses. I have already prepared the pictures and I'm looking forward to reading your opinions on them. However, there is something that needs to be discussed before.

Last Monday I was pleased to reveal the recognition this relatively young blog got from an important website such as Sciencebase.

Writing on the internet means exposing yourself to a huge audience: it can mean becoming more or less popular (Dylan's tenderbutton was, at least in my opinion, a beautiful example of what a chemical blog should be). There are certainly a few drawbacks, though: what you say is public, everyone can read it and know something about you. When it comes to blogs, moreover, there are comments: these are the best part of the story, providing a immediate feedback. Readers can show their appreciation, share their views, correct you when you are wrong and so on. 

In Italy we use to say the more the enemies, the greater the honour. In my case, I cannot say I have achieved many honours, but not everyone can be our friend, right?
Writing your own real name on your web-site is not the best way to protect your privacy, but I don't think a smart guy like Paul Docherty has ever had problems with it. Or has ever received comments on his fantastic blog dealing with his private life (spam is an issue we all have to cope with and something completely different). 

Now, yesterday, a boring person I know well (that's for you: I can see your email address, your IP and how you came here through Google. Next time, you'd better pluck up courage and sign your rubbish with your real name, eh?) posted very inappropriate comments, in the WHOIS part of the blog. It was very sad: I always hope people are intelligent and smart, or, at least, grown enough to have left their childhood by the time they go to  university. How naive, eh? 

My first reaction was to remove the WHOIS page. Now, with the benefit of hindsight, I wouldn't have made that page but, after yesterday, I can't draw back: it'll be on line, in a new version, quite soon again.
Then, I considered not allowing comments any more. It would be an easy way to solve that kind of problem. Yes, but it would be too easy. 

Finally I reached my conclusion: we go on, whether the people who don't like us like it or not. IPs can be banned, unfortunately there is no way to do the same with people's stupidity, but I don't want to damage a lot of nice people because of one or four boring ignorants. 

That's it, lads. Seeya!

Last night I drove after three months of cycling. I took some relatives to a small restaurant on the hills surrounding Bologna. I ate quite a lot, as usuall, and we had a nice time together.
By the way, the journey from home to the place wasn't that nice, since, although I like driving VERY much, a small, dark, hill road is not what you would call the easiest one for reviewing your driving skills. Nevertheless, I didn't have any trouble: I was just a little bit worried in the beginning.

It's hard to define what memory actually is: maybe the faculty of recalling facts or recognizing episodes of the past is the clearest.
Certainly, finding out all the cerebral pathaways that deal with this faculty is one of the toughest tasks of today's neuroscientists.
However, nowadays we know something.

First of all, we can define three (but there are different classifications) memories: short-term, long-term implicit and explicit memory.

Short-term memory can be called working memory as well. This second, more modern name is used to underline the functions of this kind of memory. A short-term memory, in fact, helps us every time a particular task needs a quick storage and manipulation of information/data (i.e. remembering addends for a sum and calculating the result).
Studies on monkeys and patients with brain injuries have revealed that some areas of the premotor cortex show an increases activity during processes which require the use of working memory.

When it comes to long-term memories, things get more complicated and unknown. There are five regions certainly involved: one is subcortical ( the amygdala) and the others are in the temporal cortex (namely, enthorinal, perirhinal and parahippocampal cortex, hippocampus).
Explicit memory is also called declarative memory: basically, it's when we are aware of knowing something (i.e. where we live).

Amygdala has a central role in linking memories and emotions together.

Hippocampus is nicknamed "teacher", because of its paramount importance for declarative memory. Its bidirectional connections with all the cortices explain why it plays a key role in explicit memory.
Interestingly, in the hippocampus there are staminal neurons.

Perirhinal cortex makes us remember, in a nutshell, objects, while parahippocampal cortex is linked to visuospatial memory. Both have the same bidirectional links to all the cortices we described for the hippocampus.
These two regions send information to the enthorinal cortex, which processes the inputs. Enthorinal cortex is linked to the hippocampus too and provides a huge number of inputs for it.

Implicit memory is also known as procedural memory: we know how to do something, but we are just not aware of it. And that's the link between yesterday's driving after a long time and memory. Implicit memory is what  helps us doing many things without, literally, thinking about what we are doing. For example, if we constantly had to think about how to move our legs while cycling, we would be probably fall down very quickly.
The scheme is quite simple: all cortices have connections with basal ganglia but not the way back. Hence, we can't be aware of the process.
Basal nuclei (another name for basal ganglia) receive stimuli also from the substantia nigra.
Inputs travels from basal nuclei to ventral thalmus and, finally, reach the premotor and motor cortex.

I'm proud of the way this blog is going on. Honestly, when I began, it was more because Mitch had asked me rather than a personal need.
Approximately two months later, I have definitely changed my mind: I'm so fond of this blog.

Yes, so far, I've almost lectured the readers, but things are going to change.
Today this half decent blog made a giant, significant leap towards FAME. There is a very prestigious site linking to this plucky new kid on the block: The Half Decent Pharmaceutical Chemistry Blog is now listed on Sciencebase.

For what concerns the weeks ahead, pharmaceutical chemistry is going to make his debut on these pages. And it'll have a massive impact with organic chemistry (syntheses and properties of drugs, biological pathways explained from a chemical point of view) ruling the place.

Moreover, many other themes will be discussed here, as well as those you can already find it.

As you can see, many important people already read The Half Decent Pharmaceutical Chemistry Blog.
Don't you want to join us?

Language distinguishes humans from the other hominids (chimpanzees, gorillas, and orangutans). We can point out three major aspects of language: writing, reading and speaking, which is the easiest to explain, from a nonscientific point of view.

Interestingly, languages have some points in common in every culture: every person learns it at an early stage of life and every language presents its own syntax (subject, verb and complement: what varies is the order) and grammar (every language has rules).

Towards the end of the 19th century, Paul Broca and Carl Wernicke found the two, most important areas of human brain linked to the ability to speak.
Both studied a pathology generally called aphasia (inability to speak). It has to be pointed out that aphasia can mean either the inability to understand heard words or to speak. And that made a huge difference.
The two aphasias, in fact, depends on which of the two areas has been damaged: Wernicke's or Broca's area.

Both areas are in the left brain in right handed people. In 70% percent of left handed humans, they are on the same side, while the remaining 30% is divided into a 15% who has them on the right and a 15% in both hemispheres.

Wernicke's area is in the posterior temporal lobe and surrounds the primary auditory area. That is quite obvious, because of the links between listening and speaking.
Words reach A1 and, then, Wernicke's area, which contains sound images of heard words. Hence, thanks to this area, we can comprehend the words we hear.

The information is sent to the Broca's area by the arcuate fasciculus. Broca's area is situated in the left inferior frontal region and creates those programmes for moving the organs we use to articulate words (mouth, tongue, etc.).

It has to be said that there are other parts of our brain, which are involved in speaking: the supplementary language area and some zones of motor and somatosensory cortex.

For what concerns aphasias, according to the different functions of the damaged regions, we can explain the three different types: a damage of the Wernicke's area will result in a receptive aphasia (the patient can't understand any language) and one of the Broca's area in an expressive aphasia (the patient understand what heard but won't be able to repeat it or to reply).
A problem with the auxiliary areas causes a problem of speech arrest: the patient is likely to develop a variable inability to conclude phrases.